Juprenil may be available in the countries listed below.
Selegiline hydrochloride (a derivative of Selegiline) is reported as an ingredient of Juprenil in the following countries:
International Drug Name Search
Generic Name: magnesium supplement (Oral route, Parenteral route)
In the U.S.
In Canada
Available Dosage Forms:
Magnesium is used as a dietary supplement for individuals who are deficient in magnesium. Although a balanced diet usually supplies all the magnesium a person needs, magnesium supplements may be needed by patients who have lost magnesium because of illness or treatment with certain medicines.
Lack of magnesium may lead to irritability, muscle weakness, and irregular heartbeat.
Injectable magnesium is given only by or under the supervision of a health care professional. Some oral magnesium preparations are available only with a prescription. Others are available without a prescription.
For good health, it is important that you eat a balanced and varied diet. Follow carefully any diet program your health care professional may recommend. For your specific dietary vitamin and/or mineral needs, ask your health care professional for a list of appropriate foods. If you think that you are not getting enough vitamins and/or minerals in your diet, you may choose to take a dietary supplement.
The best dietary sources of magnesium include green leafy vegetables, nuts, peas, beans, and cereal grains in which the germ or outer layers have not been removed. Hard water has been found to contain more magnesium than soft water. A diet high in fat may cause less magnesium to be absorbed. Cooking may decrease the magnesium content of food.
The daily amount of magnesium needed is defined in several different ways.
Normal daily recommended intakes in milligrams (mg) for magnesium are generally defined as follows:
| Persons | U.S. (mg) | Canada (mg) |
| Infants birth to 3 years of age | 40 to 80 | 20–50 |
| Children 4 to 6 years of age | 120 | 65 |
| Children 7 to 10 years of age | 170 | 100–135 |
| Adolescent and adult males | 270–400 | 130–250 |
| Adolescent and adult females | 280–300 | 135–210 |
| Pregnant females | 320 | 195–245 |
| Breast-feeding females | 340–355 | 245–265 |
If you are taking a dietary supplement without a prescription, carefully read and follow any precautions on the label. For these supplements, the following should be considered:
Tell your doctor if you have ever had any unusual or allergic reaction to medicines in this group or any other medicines. Also tell your health care professional if you have any other types of allergies, such as to foods dyes, preservatives, or animals. For non-prescription products, read the label or package ingredients carefully.
Problems in children have not been reported with intake of normal daily recommended amounts.
Problems in older adults have not been reported with intake of normal daily recommended amounts.
Studies have shown that older adults may have lower blood levels of magnesium than younger adults. Your health care professional may recommend that you take a magnesium supplement.
It is especially important that you are receiving enough vitamins and minerals when you become pregnant and that you continue to receive the right amount of vitamins and minerals throughout your pregnancy. The healthy growth and development of the fetus depend on a steady supply of nutrients from the mother. However, taking large amounts of dietary supplements during pregnancy may be harmful to the mother and/or fetus and should be avoided.
It is especially important that you receive the right amount of vitamins and minerals so that your baby will also get the vitamins and minerals needed to grow properly. However, taking large amounts of a dietary supplement while breast-feeding may be harmful to the mother and/or baby and should be avoided.
Although certain medicines should not be used together at all, in other cases two different medicines may be used together even if an interaction might occur. In these cases, your doctor may want to change the dose, or other precautions may be necessary. When you are taking any of these dietary supplements, it is especially important that your healthcare professional know if you are taking any of the medicines listed below. The following interactions have been selected on the basis of their potential significance and are not necessarily all-inclusive.
Using dietary supplements in this class with any of the following medicines is usually not recommended, but may be required in some cases. If both medicines are prescribed together, your doctor may change the dose or how often you use one or both of the medicines.
Certain medicines should not be used at or around the time of eating food or eating certain types of food since interactions may occur. Using alcohol or tobacco with certain medicines may also cause interactions to occur. Discuss with your healthcare professional the use of your medicine with food, alcohol, or tobacco.
The presence of other medical problems may affect the use of dietary supplements in this class. Make sure you tell your doctor if you have any other medical problems, especially:
This section provides information on the proper use of a number of products that contain magnesium supplement. It may not be specific to Maginex. Please read with care.
Magnesium supplements should be taken with meals. Taking magnesium supplements on an empty stomach may cause diarrhea.
For individuals taking the extended-release form of this dietary supplement:
For individuals taking the powder form of this dietary supplement:
The dose medicines in this class will be different for different patients. Follow your doctor's orders or the directions on the label. The following information includes only the average doses of these medicines. If your dose is different, do not change it unless your doctor tells you to do so.
The amount of medicine that you take depends on the strength of the medicine. Also, the number of doses you take each day, the time allowed between doses, and the length of time you take the medicine depend on the medical problem for which you are using the medicine.
If you miss a dose of this medicine, take it as soon as possible. However, if it is almost time for your next dose, skip the missed dose and go back to your regular dosing schedule. Do not double doses.
If you miss taking your magnesium supplement for one or more days there is no cause for concern, since it takes some time for your body to become seriously low in magnesium. However, if your health care professional has recommended that you take magnesium, try to remember to take it as directed every day.
Keep out of the reach of children.
Store the medicine in a closed container at room temperature, away from heat, moisture, and direct light. Keep from freezing.
Do not keep outdated medicine or medicine no longer needed.
Along with its needed effects, a medicine may cause some unwanted effects. Although not all of these side effects may occur, if they do occur they may need medical attention.
Check with your doctor immediately if any of the following side effects occur:
Some side effects may occur that usually do not need medical attention. These side effects may go away during treatment as your body adjusts to the medicine. Also, your health care professional may be able to tell you about ways to prevent or reduce some of these side effects. Check with your health care professional if any of the following side effects continue or are bothersome or if you have any questions about them:
Other side effects not listed may also occur in some patients. If you notice any other effects, check with your healthcare professional.
Call your doctor for medical advice about side effects. You may report side effects to the FDA at 1-800-FDA-1088.
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Class: Class Ib Antiarrhythmics
Molecular Formula: C25H28N6O3S•½C4H4 O4
CAS Number: 6108-05-0
Antiarrhythmic agent; an amide-type local anesthetic, class IB agent.a
Alternative to other antiarrhythmic drugs (e.g., amiodarone, procainamide, sotalol) for the acute treatment of hemodynamically compromising ventricular ectopy (e.g., VPCs) that occurs following myocardial ischemia or infarction or during cardiac manipulative procedures such as cardiac surgery or cardiac catheterization.121 123 128
Prophylactic use to reduce primary VF following AMI is not recommended.121 123 128
Alternative antiarrhythmic agent to amiodarone in the treatment of cardiac arrest secondary to VF or pulseless VT resistant to CPR, cardioversion (e.g., after 2 to 3 shocks) and a vasopressor (epinephrine, vasopressin).121 123 128
Alternative to other antiarrhythmic agents or synchronized electrical cardioversion in the treatment of hemodynamically stable monomorphic VT in patients with preserved ventricular function;123 128 however, other agents are preferred.128
Alternative antiarrhythmic agent in the treatment of hemodynamically stable polymorphic VT in patients with normal baseline QT interval and preserved ventricular function (when ischemia is treated and electrolyte imbalance is corrected) or with prolonged baseline QT interval that suggests torsades de pointes;123 128 efficacy not established in torsades de pointes.128
Drug-induced cardiovascular emergencies or altered vital signs: May consider use in tachycardia, impaired conduction/ventricular arrhythmias, hypertensive emergencies, or acute coronary syndrome associated with stimulants (e.g., amphetamine, methamphetamine, cocaine, phencyclidine, ephedrine), tricyclic antidepressant, cardiac glycoside, or class I antiarrhythmic (e.g., procainamide, disopyramide, propafenone, flecainide) toxicity; do not use in lidocaine overdose.128 Safety and efficacy not established in drug-induced polymorphic VT.128 Efficacy not established in torsades de pointes.128
Treatment of status epilepticus†, as a last resort.a
Solutions containing epinephrine must not be used to treat arrhythmias.a
Adjust dosage carefully according to individual requirements and response;b constant ECG monitoring is recommended.b
Discontinue therapy for VF or VT (at least temporarily) after 6–24 hours to reassess ongoing need for antiarrhythmic drugs.121 Terminate infusion as soon as the basic cardiac rhythm appears to be stable or at the earliest sign of toxicity.a Immediately stop infusion if signs of excessive cardiac depression occur (e.g., prolongation of PR interval and QRS complex, appearance or aggravation of arrhythmias).b
Infusions continued for >24 hours should be rarely necessary.b
Administer IV.a Has been administered IM (no longer commercially available in the US); IV infusion is preferred.a
For ACLS during CPR, may be administered via endotracheal tube† or by intraosseous injection† when IV administration is not possible.124 128 Although endotracheal† administration is possible, IV or intraosseous† administration is preferred because of more predictable drug delivery and pharmacologic effect.128
For solution and drug compatibility information, see Compatibility under Stability.
Administer as a bolus IV injection for initial treatment of ventricular arrhythmias.a Maintenance IV infusions may be required to maintain normal sinus rhythm if oral antiarrhythmic therapy is not feasible.a
Administer via a peripheral vein (antecubital or external jugular in adults and the largest most accessible vein that does not interrupt resuscitation in pediatric patients) during CPR when a vein has not been cannulated prior to the arrest, since central venous access requires interruption of chest compressions, is technically more difficult, and is associated with an increased risk of complications.123 124 128
Administer via a central venous catheter (if already in place at the time of arrest) because of more rapid onset of drug activity (in adults),123 128 more secure access to circulation, and avoidance of tissue infiltration.124 128
Avoid central venous line placement in candidates for pharmacologic reperfusion (e.g., with thrombolytic therapy) and/or fibrinolytic therapy.123 128
Injections containing preservatives should not be given IV.a
Do not introduce additives into solutions of lidocaine in 5% dextrose, since dosage is titrated to response.b
Do not add to blood transfusion assemblies.a
Do not use commercially available solutions of lidocaine in 5% dextrose in series connections with other plastic containers; such use could result in air embolism.a
Lidocaine hydrochloride injections containing 40, 100, or 200 mg/mL are for the preparation of IV infusion solutions and must be diluted prior to administration. Massive overdosage resulting in cardiac arrest, seizures, and/or death may occur if administered by direct IV administration without prior dilution.a
Prepare IV infusions by adding 1 g of lidocaine hydrochloride (25 mL of 4% or 5 mL of 20% lidocaine hydrochloride injection) to 1 L of 5% dextrose injection to provide a solution containing 1 mg/mL.a
Alternatively, use commercially available 0.4 or 0.8% solutions in 5% dextrose.a
If fluid restriction is desirable, up to 8 mg/mL may be used.b
Administer IV bolus dose at a rate of 25–50 mg/minute (0.35–0.7 mg/kg per minute).100 121 123 128
Administer maintenance infusions at a rate of 20–50 mcg/kg per minute in adults or 10–50 mcg/kg per minute in pediatric patients.a b
For other populations, see Special Populations under Dosage and Administration.
For intraosseous injection, place a cannula in a noncollapsible marrow venous plexus using a rigid needle, preferably a specially designed intraosseous or Jamshidi-type bone marrow needle; a styleted needle is preferred to prevent obstruction of the needle with cortical bone.124
Insert intraosseous needle into the anterior tibial bone marrow; alternatively, the distal femur, medial malleolus, or anterior superior iliac spine can be used.124 In older children and adults, intraosseous cannulas may be inserted into the distal radius or ulna in addition to the proximal tibia.124
For administration via endotracheal tube, dilute dose in 5–10 mL of 0.9% sodium chloride or sterile water (for adults)123 128 or flush with a minimum of 5 mL of 0.9% sodium chloride followed by 5 assisted manual ventilations (for pediatric patients).124 128 Dilution in sterile water may increase absorption of lidocaine;123 128 however, sterile water may have a more negative effect on arterial oxygen pressure (PaO2).123
Available as lidocaine hydrochloride; dosage is expressed in terms of the salt.a
Initially, 0.5–1 mg/kg as a rapid IV injection (i.e., bolus); dose may be repeated according to patient response, up to a maximum total dose of 3–5 mg/kg.a Maintenance infusion of 10–50 mcg/kg per minute.a
For ACLS, 1 mg/kg initially, up to maximum initial dose of 100 mg.106 124 128 129 If VT or VF is not corrected following defibrillation (or cardioversion) and initial lidocaine dose, give 20–50 mcg/kg per minute as an IV infusion.124 128 If the time between initial IV bolus dose and onset of IV infusion exceeds 15 minutes, give an additional IV bolus of 0.5–1 mg/kg.106 124
Initially, 1 mg/kg, up to maximum initial dose of 100 mg.106 124 128 129 If VT or VF is not corrected following defibrillation (or cardioversion) and initial lidocaine dose, give infusion of 20–50 mcg/kg per minute.124 128
Optimal dose not established.128
Initially, 2–3 mg/kg;106 124 128 130 however, 2–2.5 times the recommended IV dosage may be recommended.124 128
Initial doses ranging from 0.5–0.75 mg/kg and up to 1–1.5 mg/kg (about 50–100 mg) administered as rapid IV injection may be used.100 128 If desired response is not achieved, 25–50 mg may be administered 5 minutes after completion of the first injection,100 or 0.5–0.75 mg/kg as rapid IV injection may be repeated at 5- to 10-minute intervals as necessary, up to a total of 3 doses (or up to 3 mg/kg).121 123 128
Cardiac arrest secondary to VF or pulseless VT: 1–1.5 mg/kg as initial loading dose,121 123 128 then 0.5–0.75 mg/kg as rapid IV injection repeated at 5- to 10-minute intervals as necessary, up to a total of 3 doses (or up to 3 mg/kg).121 123 128
Maintenance infusion of 30–50 mcg/kg per minute (1–4 mg/minute in an average 70-kg adult).128
If arrhythmias recur during maintenance infusion, administer 0.5 mg/kg as a bolus dose while maintaining or increasing infusion rate simultaneously up to a maximum rate of 4 mg/minute.123
Cardiac arrest secondary to VF or pulseless VT: 1–1.5 mg/kg as initial loading dose, then 0.5–0.75 mg/kg repeated at 5- to 10-minute intervals as necessary, up to a total of 3 doses (or up to 3 mg/kg).128
Optimal dose not established.128
Usually, 2–2.5 times the recommended IV dosage.123 128
Initially, 1 mg/kg.a After 2 minutes, administer 0.5 mg/kg if seizure is not terminated.a Maintenance infusion of 30 mcg/kg per minute for prevention of seizure recurrence.a
Maximum 3–5 mg/kg for initial treatment.a
ACLS: 1 mg/kg initially up to maximum initial dose of 100 mg.128 129
ACLS: 1 mg/kg initially up to maximum initial dose of 100 mg.128 129
Maximum 3 mg/kg as total dose for initial treatment.121 123 128
Maximum total dose of 200–300 mg over a 1-hour period.100
Maximum 4 mg/minute as maintenance infusion.123 128
Careful and individualized dosing recommended.32 107 108 109 110 111 112 113 114 115 116
Slower infusion rates (e.g., 50% of usual maintenance infusion) recommended.123
Reduce infusion rate after 24 hours to 1–2 mg/minute; dosage reduction may be guided by plasma lidocaine concentrations.121
Dosage modification not required.a
Slower infusion rates (e.g., 50% of usual maintenance infusion) recommended in patients >70 years of age.123
Smaller bolus doses may be required.a
Slower infusion rates (e.g., 50% of usual maintenance infusion) recommended in patients with decreased cardiac output (e.g., hypotension or shock associated with AMI, poor peripheral perfusion states, CHF).123
Maximum infusion rate of 20 mcg/kg per minute in patients with persistently poor cardiac output and hepatic or renal failure;124 <30 mcg/kg per minute in patients with CHF.a
Reduce infusion rate after 24 hours to 1–2 mg/minute; dosage reduction may be guided by plasma lidocaine concentrations.121
Possible increased half-life following infusions lasting>24 hours; reduce dosage accordingly (e.g., by 50%) to avoid accumulation of the drug and potential toxicity.a
Adams-Stokes syndrome; severe degrees of SA, AV, or intraventricular heart block (unless a functioning pacemaker is present).b Some manufacturers state that lidocaine is contraindicated in patients with Wolff-Parkinson-White syndrome.b
Known hypersensitivity to amide-type local anesthetics.b
Constant ECG monitoring is necessary during IV administration.b Discontinue infusion if signs of excessive cardiac depression occur (e.g., prolongation of PR interval and QRS complex, appearance or aggravation of arrhythmias).b
Resuscitative equipment and drugs should be immediately available for the management of severe adverse cardiovascular, respiratory, or CNS effects.b Discontinue therapy if severe reactions occur; institute emergency resuscitative procedures and other supportive measures as required.a b
Severe reactions may be preceded by somnolence and paresthesia.a
Possible hypersensitivity reactions (e.g., skin lesions, urticaria, edema, anaphylactoid reactions).a
Possible increased half-life following infusions lasting >24 hours; reduce dosage accordingly (see Patients Requiring Prolonged Therapy under Dosage and Administration).a
If maintenance therapy is necessary, an oral antiarrhythmic agent (e.g., procainamide) is recommended.a
Possible muscle twitching or tremors, seizures, unconsciousness, and coma;a b 128 may be associated with high doses or overdosage.b
Possible drowsiness, disorientation, slurred speech, and altered consciousness.128
Possible hypotension, arrhythmias, heart block, cardiovascular collapse, and bradycardia,a b 128 which may lead to cardiac arrest in patients with high plasma lidocaine concentrations or myocardial conduction defects.a b
Possible serious ventricular arrhythmias or heart block in patients with sinus bradycardia;a potentially life-threatening adverse effects in patients with symptomatic bradycardia.123
Possible increased sensitivity to cardiac depressant effects in patients with a diseased or abnormal sinus node.a
Possible increased ventricular rate in patients with atrial fibrillation.a
Possible increased coronary blood flow in patients with recent MI.a
Possible myocardial and circulatory depression.128
Cautious use recommended in patients with any form of heart block, CHF, marked hypoxia, severe respiratory depression, hypovolemia, or shock.a
Possible respiratory depression and arrest;a b may be associated with high doses or overdosage.b
Possible local thrombophlebitis in patients receiving prolonged IV infusions.a
Tissue infiltration may lead to local ischemia, tissue injury, and ulceration.128
Possible increased serum CK (CPK) concentrations associated with IM injections.a Isoenzyme separation is necessary when CK determinations are used in the diagnosis of AMI.a
Category B.b
Distributed into milk.117 Use with caution.100
Safety and efficacy not established in controlled clinical studies;100 however, lidocaine has been used for treatment of ventricular arrhythmias in infants and children.123 128
Use may be considered in children as an alternative antiarrhythmic agent, if amiodarone is unavailable, in the treatment of cardiac arrest secondary to VF or pulseless VT resistant to CPR, cardioversion, and epinephrine.124 128
Use with caution.a (See Pharmacokinetics and also see Hepatic Impairment under Dosage and Administration.)
Use with caution in severe renal impairment.a (See Elimination: Special Populations, under Pharmacokinetics.)
Adverse CNS effects (e.g., drowsiness, dizziness, disorientation, confusion, lightheadedness, tremulousness, psychosis, nervousness, apprehension, agitation, euphoria, tinnitus, visual disturbances, paresthesia, difficulty swallowing, dyspnea, slurred speech, sensations of heat, cold, or numbness), nausea, vomiting.b
Potential pharmacologic interaction (additive or antagonistic cardiac effects and additive toxicity) with concomitant administration of antiarrhythmic agents (e.g., phenytoin, procainamide, propranolol, quinidine).a
Drug | Interaction | Comments |
|---|---|---|
Cimetidine | Decreased lidocaine clearancea | Monitor serum lidocaine concentrations and observe closely for signs of lidocaine toxicitya |
Phenytoin | Possible increased lidocaine metabolismb | Clinical importance unknownb |
Propranolol | Decreased lidocaine clearancea | Monitor serum lidocaine concentrations and observe closely for signs of lidocaine toxicitya |
Succinylcholine | Increased neuromuscular blocking effecta | Appears to be important only at lidocaine doses higher than those used clinicallya |
Absorbed from the GI tract, but passes into hepatic circulation and only about 35% of an oral dose reaches the systemic circulation unchanged.a Toxic effects appear at oral doses that fail to produce therapeutic plasma concentrations.a
Following IM (deltoid) injection, peak plasma concentrations are achieved in 10 minutes.a
Following direct IV (bolus) administration of 50–100 mg, onset of action is 45–90 seconds.a
Following direct IV (bolus) administration of 50–100 mg, duration is 10–20 minutes.a
Plasma lidocaine concentrations of 1–5 mcg/mL are required to suppress ventricular arrhythmias; concentrations exceeding 5 mcg/mL associated with toxicity.a
Widely distributed into body tissues.a Readily crosses the blood-brain barrier.117 Crosses the placenta and is distributed into milk.117
Early, rapid decline in plasma concentrations is associated with distribution into highly perfused tissues (e.g., kidneys, lungs, liver, heart);a slower elimination phase associated with metabolism and redistribution into skeletal muscle and adipose tissue.a
Binding is variable and concentration dependent;100 101 102 103 104 105 60 –80% bound to plasma proteins at concentrations of 1–4 mcg/mL.100 101 102 103 104 105 Partially bound to α1-acid glycoprotein.100 102 103 104 105
Volume of distribution is decreased in patients with CHF and increased in patients with liver disease.a
Approximately 90% of a parenteral dose is metabolized rapidly in the liver by de-ethylation to the active metabolites monoethylglycinexylidide (MEGX) and glycinexylidide (GX).a Rate of metabolism appears to be limited by hepatic blood flow.a
Excreted in urine principally as metabolites.a
Lidocaine has an initial half-life of 7–30 minutes and a terminal half-life of 1.5–2 hours.a Elimination half-lives of MEGX and GX are 2 and 10 hours, respectively.a
Rate of metabolism of lidocaine may be decreased and the half-life increased in patients with liver disease.a Major differences may exist in pharmacokinetics for different types of liver disease (e.g., cirrhosis, hepatitis); no consistent correlation established between clearance and severity of liver disease (as determined by liver function tests).32 107 108 109 110 111 112 113 114 115 116
GX may accumulate in patients with renal failure.a
In patients with MI, the half-lives of lidocaine and its metabolites appear to be prolonged.a
In patients with CHF, half-life of lidocaine may be prolonged.a
In individuals receiving continuous IV infusions lasting >24 hours, half-life of lidocaine may be prolonged.a
25°C; may be exposed briefly to temperatures up to 40°C.a Do not freeze; protect from excessive heat.a
Extemporaneously prepared solutions (1–4 mg/mL in 5% dextrose injection) appear to be stable at room temperature for at least 24 hours.a
For information on systemic interactions resulting from concomitant use, see Interactions.
Compatible |
|---|
Amino acids 4.25%, dextrose 25% |
Dextrose 5% in Ringer’s injection, lactated |
Dextrose 5% in sodium chloride 0.45 or 0.9% |
Dextrose 5% in water |
Ringer’s injection, lactated |
Sodium chloride 0.45 or 0.9% |
Drugs that require low pH for stability (e.g., dopamine, epinephrine, norepinephrine, isoproterenol) may be adversely affected by the pH of lidocaine (5–7).a Use such mixtures promptly after preparation or consider separate administration of the drugs.a The manufacturers state that commercially available solutions of lidocaine hydrochloride in 5% dextrose should not be mixed with other drugs.a b
Compatible |
|---|
Alteplase |
Aminophylline |
Amiodarone HCl |
Atracurium besylate |
Bretylium tosylate |
Calcium chloride |
Calcium gluconate |
Chloramphenicol sodium succinate |
Chlorothiazide sodium |
Cimetidine HCl |
Ciprofloxacin |
Dexamethasone sodium phosphate |
Digoxin |
Diphenhydramine HCl |
Dobutamine HCl |
Dopamine HCl |
Ephedrine sulfate |
Erythromycin lactobionate |
Flumazenil |
Furosemide |
Heparin sodium |
Hydrocortisone sodium succinate |
Hydroxyzine HCl |
Mephentermine sulfate |
Metaraminol bitartrate |
Nafcillin sodium |
Nitroglycerin |
Penicillin G potassium |
Pentobarbital sodium |
Phenylephrine HCl |
Potassium chloride |
Procainamide HCl |
Prochlorperazine edisylate |
Propafenone HCl |
Ranitidine HCl |
Sodium bicarbonate |
Sodium lactate |
Theophylline |
Verapamil HCl |
Vitamin B complex with C |
Incompatible |
Methohexital sodium |
Phenytoin sodium |
Variable |
Fentanyl citrate |
Compatible |
|---|
Alteplase |
Amiodarone HCl |
Bivalirudin |
Cefazolin sodium |
Ciprofloxacin |
Clarithromycin |
Daptomycin |
Dexmedetomidine HCl |
Diltiazem HCl |
Dobutamine HCl |
Dobutamine HCl with dopamine HCl |
Dobutamine HCl with nitroglycerin |
Dobutamine HCl with sodium nitroprusside |
Dopamine HCl |
Dopamine HCl with dobutamine HCl |
Dopamine HCl with nitroglycerin |
Dopamine HCl with sodium nitroprusside |
Enalaprilat |
Etomidate |
Famotidine |
Fenoldopam mesylate |
Haloperidol lactate |
Heparin sodium |
Heparin sodium with hydrocortisone sodium succinate |
Hetastarch in lactated electrolyte injection (Hextend) |
Inamrinone lactate |
Labetalol HCl |
Levofloxacin |
Linezolid |
Meperidine HCl |
Morphine sulfate |
Nicardipine HCl |
Nitroglycerin |
Nitroglycerin with dobutamine HCl |
Nitroglycerin with dopamine HCl |
Nitroglycerin with sodium nitroprusside |
Potassium chloride |
Propofol |
Remifentanil HCl |
Sodium nitroprusside |
Sodium nitroprusside with dobutamine HCl |
Sodium nitroprusside with dopamine HCl |
Sodium nitroprusside with nitroglycerin |
Streptokinase |
Theophylline |
Tirofiban HCl |
Vasopressin |
Vitamin B complex with C |
Warfarin sodium |
Incompatible |
Amphotericin B cholesteryl sulfate complex |
Lansoprazole |
Thiopental sodium |
Membrane-stabilizing antiarrhythmic agent.a Combines with fast sodium channels in their inactive state and inhibits recovery after repolarization in a time- and voltage-dependent manner.a Exhibits rapid rates of attachment to and dissociation from transmembrane sodium channels.a
Controls ventricular arrhythmias by suppressing automaticity in His-Purkinje system and by suppressing spontaneous depolarization of the ventricles during diastole.a b 128
Little effect on AV node conduction and His-Purkinje conduction in normal heart at therapeutic concentrations.a Affects conducting tissues of ventricles more than atria.a Variable effect on the effective refractory period (ERP) of the AV node; ERP and action potential duration of the His-Purkinje system are shortened.a
Cardiac actions appear to be similar to those of phenytoin.a
CNS depressant.a Produces sedative, analgesic, and anticonvulsant effects.a Suppresses cough and gag reflexes.a
Produces little effect on autonomic tone; generally does not produce a substantial fall in BP, decreased myocardial contractility, or diminished cardiac output.a Usually has little effect on heart rate.a
Importance of informing clinicians of existing or contemplated concomitant therapy, including prescription and OTC drugs, and of concomitant illnesses.a
Importance of women informing clinicians if they are or plan to become pregnant or plan to breast-feed.b
Importance of advising patients of other important precautionary information.b (See Cautions.)
Excipients in commercially available drug preparations may have clinically important effects in some individuals; consult specific product labeling for details.
* available from one or more manufacturer, distributor, and/or repackager by generic (nonproprietary) name
Routes | Dosage Forms | Strengths | Brand Names | Manufacturer |
|---|---|---|---|---|
Parenteral | Injection, for direct IV injection | 10 mg/mL* | Lidocaine Hydrochloride Injection for Cardiac Arrhythmias | |
20 mg/mL* | Lidocaine Hydrochloride Injection for Cardiac Arrhythmias | |||
Injection, for preparation of IV infusion only | 100 mg/mL (1 g)* | Lidocaine Hydrochloride Injection for Cardiac Arrhythmias | ||
200 mg/mL (1 or 2 g)* | Lidocaine Hydrochloride Injection for Cardiac Arrhythmias |
* available from one or more manufacturer, distributor, and/or repackager by generic (nonproprietary) name
Routes | Dosage Forms | Strengths | Brand Names | Manufacturer |
|---|---|---|---|---|
Parenteral | Injection, for IV infusion | 4 mg/mL (1 or 2 g) Lidocaine Hydrochloride in 5% Dextrose* | 0.4% Lidocaine Hydrochloride and 5% Dextrose Injection (LifeCare and glass containers [Hospira], Viaflex [Baxter], Excel [Braun]) | |
8 mg/mL (2 or 4 g) Lidocaine Hydrochloride in 5% Dextrose* | 0.8% Lidocaine Hydrochloride and 5% Dextrose Injection (LifeCare [Hospira], Viaflex [Baxter], Excel [Braun]) |
This report on medications is for your information only, and is not considered individual patient advice. Because of the changing nature of drug information, please consult your physician or pharmacist about specific clinical use.
The American Society of Health-System Pharmacists, Inc. and Drugs.com represent that the information provided hereunder was formulated with a reasonable standard of care, and in conformity with professional standards in the field. The American Society of Health-System Pharmacists, Inc. and Drugs.com make no representations or warranties, express or implied, including, but not limited to, any implied warranty of merchantability and/or fitness for a particular purpose, with respect to such information and specifically disclaims all such warranties. Users are advised that decisions regarding drug therapy are complex medical decisions requiring the independent, informed decision of an appropriate health care professional, and the information is provided for informational purposes only. The entire monograph for a drug should be reviewed for a thorough understanding of the drug's actions, uses and side effects. The American Society of Health-System Pharmacists, Inc. and Drugs.com do not endorse or recommend the use of any drug. The information is not a substitute for medical care.
AHFS Drug Information. © Copyright, 1959-2011, Selected Revisions August 2007. American Society of Health-System Pharmacists, Inc., 7272 Wisconsin Avenue, Bethesda, Maryland 20814.
† Use is not currently included in the labeling approved by the US Food and Drug Administration.
Only references cited for selected revisions after 1984 are available electronically.
32. Thomson PD, Melmon KL, Richardson JA et al. Lidocaine pharmacokinetics in advanced heart failure, liver disease, and renal failure in humans. Ann Intern Med. 1973; 78:499-508. [IDIS 31055] [PubMed 4694036]
52. Anon. Lignocaine for acute ventricular arrhythmias. Drug Ther Bull. 1969; 7:5-6. [PubMed 5763260]
100. Astra Pharmaceutical Products, Inc. Xylocaine (lidocaine hydrochloride) solution for ventricular arrhythmias prescribing information. Westborough, MA; 1997 Jun.
101. Tucker GT, Boyes RN, Bridenbaugh PO et al. Binding of anilide-type local anesthetics in human plasma. I. Relationships between binding, physiochemical properties and anesthetic activity. Anesthesiology. 1970; 33:287-303. [PubMed 5454949]
102. Routledge PA, Barchowsky A, Bjornsson TD et al. Lidocaine plasma protein binding. Clin Pharmacol Ther. 1980; 27:347-51. [IDIS 113908] [PubMed 7357791]
103. Routledge PA, Stargel WW, Wagner GS et al. Increased alpha-1-acid glycoprotein and lidocaine disposition in myocardial infarction. Ann Intern Med. 1980; 93:701-4. [IDIS 124049] [PubMed 7212479]
104. Routledge PA, Shand DG, Barchowsky A et al. Relationship between α1-acid glycoprotein and lidocaine disposition in myocardial infarction. Clin Pharmacol Ther. 1981; 30:154-7. [IDIS 136577] [PubMed 7249498]
105. Shand DG. α1-Acid glycoprotein and plasma lidocaine binding. Clin Pharmacokinet. 1984; 9(Suppl 1):27-31. [IDIS 181413] [PubMed 6705424]
106. Standards and Guidelines for Cardiopulmonary Resuscitation (CPR) and Emergency Cardiac Care (ECC). JAMA. 1986; 255:2905-84.
107. Forrest JAH, Finlayson NDC, Adjepon-Yamoah KK et al. Antipyrine, paracetamol, and lignocaine elimination in chronic liver disease. Br Med J. 1977; 1:1384-7. [PubMed 861646]
108. Williams RL, Blaschke TF, Meffin PJ et al. Influence of viral hepatitis on the disposition of two compounds with high hepatic clearance: lidocaine and indocyanine green. Clin Pharmacol Ther. 1976; 20:290-9. [PubMed 954351]
109. Selden R, Sasahara AA. Central nervous system toxicity induced by lidocaine: report of a case in a patient with liver disease. JAMA. 1967; 202:908-9. [PubMed 6072663]
110. Waller ES. Pharmacokinetic principles of lidocaine dosing in relation to disease state. J Clin Pharmacol. 1981; 21:181-94. [IDIS 158243] [PubMed 7240439]
111. Williams RL. Drug administration in hepatic disease. N Engl J Med. 1983; 309:1616-22. [IDIS 179500] [PubMed 6358891]
112. Rodman JH. Lidocaine. In: Evans WE, Schentag JJ, Jusko WJ, eds. Applied pharmacokinetics: principles of therapeutic drug monitoring. San Francisco: Applied Therapeutics, Inc; 1980:350-91.
113. Pomier-Layrargues G, Huet PM, Villeneuve JP et al. Effect of portacaval shunt on drug disposition in patients with cirrhosis. Gastroenterology. 1986; 91:163-7. [IDIS 217341] [PubMed 3710065]
114. Villeneuve JP, Thibeault MJ, Ampelas M et al. Drug disposition in patients with HBsAg-positive chronic liver disease. Dig Dis Sci. 1987; 32:710-4. [IDIS 232435] [PubMed 3595383]
115. Adjepon-Yamoah KK, Nimmo J, Prescott LF. Gross impairment of hepatic drug metabolism in a patient with chronic liver disease. Br Med J. 1974; 4:387-8. [PubMed 4425889]
116. Huet PM, Lelorier J. Effects of smoking and chronic hepatitis B on lidocaine and indocyanine green kinetics. Clin Pharmacol Ther. 1980; 28:208-15. [IDIS 121469] [PubMed 7398188]
117. Zeisler JA, Gaarder TD, De Mesquita SA. Lidocaine excretion in breast milk. Drug Intell Clin Pharm. 1986; 20:691-3. [IDIS 220636] [PubMed 3757781]
118. American College of Cardiology and American Heart Association. ACC/AHA guidelines for the early management of patients with acute myocardial infarction: a report of the American College of Cardiology/American Heart Association Task Force on Assessment of Diagnostic and Therapeutic Cardiovascular Procedures (Subcommittee to Develop Guidelines for the Early Management of Patients with Acute Myocardial Infarction.). Circulation. 1990; 82:664-707. [IDIS 269868] [PubMed 2197021]
119. MacMahon S, Collins R, Peto R et al. Effects of prophylactic lidocaine in suspected acute myocardial infarction: an overview of results from the randomized, controlled trials. JAMA. 1988; 260:1910-6. [IDIS 246138] [PubMed 3047448]
120. Davison R, Parker M, Atkinson AJ Jr. Excessive serum lidocaine levels during maintenance infusions: mechanisms and prevention. Am Heart J. 1982; 104:203-8. [IDIS 156217] [PubMed 7102503]
121. Ryan TJ, Antman EM, Brooks NH et al. ACC/AHA guidelines for the management of patients with acute myocardial infarction: 1999 update: a report of the American College of Cardiology/American Heart Association Task Force on Practice Guidelines (Committee on Management of Acute Myocardial Infarction). From and .
122. American Heart Association Emergency Cardiac Care Committee and Subcommittees. Guidelines for cardiopulmonary resuscitation and emergency cardiac care. Part III: adult advanced cardiac life support. JAMA. 1992; 268:2199-241. [IDIS 303939] [PubMed 1404769]
123. American Heart Association in collaboration with the International Liaison Committee on Resuscitation. Guidelines 2000 for cardiopulmonary resuscitation and emergency cardiovascular care. Part 6: advanced cardiovascular life support. Circulation. 2000;102(Suppl I):I86-171.
Class: HIV Protease Inhibitors
VA Class: AM800
Chemical Name: [3S-[2[1R*(R*),2S*],3α,4aβ,8aα]]-N1-[3-[3-[[(1,1-dimethyleth yl)amino]carbonyl]octahydro-2(1H)-isoquinolinyl]-2-hydroxy- 1-(phenylmethyl)propyl]-2-[(2-quinolinylcarbonyl)amino]-butanediamide
CAS Number: 127779-20-8
Brands: Invirase
REMS:
FDA approved a REMS for saquinavir to ensure that the benefits of a drug outweigh the risks. However, FDA later rescinded REMS requirements. See the FDA REMS page () or the ASHP REMS Resource Center ().
Antiretroviral; HIV protease inhibitor (PI).1 6 8 10 28 32 51
Treatment of HIV infection in conjunction with other antiretrovirals.1 3 6 17 20 21 48 51
Used in conjunction with low-dose ritonavir (ritonavir-boosted saquinavir) or with the fixed combination of lopinavir/ritonavir.1 130 178 179 185 186
Used in PI-based regimens that include a PI and 2 nucleoside reverse transcriptase inhibitors (NRTIs).130
For initial treatment in HIV-infected adults and adolescents, some experts state that ritonavir-boosted saquinavir is an alternative PI (not a preferred PI) for use in PI-based regimens in conjunction with 2 NRTIs.130
Postexposure prophylaxis of HIV infection† in health-care workers and others exposed occupationally via percutaneous injury or mucous membrane or nonintact skin contact with blood, tissues, or other body fluids associated with risk for transmission of the virus.117 Used in conjunction with other antiretrovirals.117
Postexposure prophylaxis of HIV infection† in individuals who have had nonoccupational exposure to blood, genital secretions, or other potentially infectious body fluids of a person known to be infected with HIV when that exposure represents a substantial risk for HIV transmission.174 Used in conjunction with other antiretrovirals.174
Administer orally within 2 hours of a meal.1 15 51
Must be used in conjunction with low-dose ritonavir (either as ritonavir-boosted saquinavir or in conjunction with fixed combination of lopinavir/ritonavir).1 130 Saquinavir should be taken at the same time as ritonavir.1
Available as saquinavir mesylate; dosage expressed as saquinavir.1
Must be given in conjunction with other antiretrovirals.1 If used with nelfinavir, dosage adjustment recommended.1 130 (See Specific Drugs and Foods under Interactions.)
Adolescents ≥16 years of age: 1 g twice daily in conjunction with low-dose ritonavir (100 mg twice daily).1 130 Alternatively, 1 g twice daily in conjunction with usual dosage of lopinavir/ritonavir twice daily.1 130
1 g twice daily in conjunction with low-dose ritonavir (100 mg twice daily).1 130 Alternatively, 1 g twice daily in conjunction with usual dosage of lopinavir/ritonavir twice daily.1 130
1 g twice daily with low-dose ritonavir (100 mg twice daily).117
Initiate postexposure prophylaxis as soon as possible following exposure (within hours rather than days) and continue for 4 weeks, if tolerated.117
1 g twice daily in conjunction with low-dose ritonavir (100 mg twice daily) or, alternatively, 400 mg twice daily in conjunction with low-dose ritonavir (400 mg twice daily).174
Initiate postexposure prophylaxis as soon as possible following exposure (preferably ≤72 hours after exposure) and continue for 28 days.174
Dosage recommendations not available; use with caution in mild to moderate hepatic impairment.1 Contraindicated in severe hepatic impairment.1
No initial dosage adjustment needed.1 Use with caution in severe renal impairment.1
Select dosage with caution because of age-related decreases in hepatic, renal, and/or cardiac function and concomitant disease and drug therapy.1
Hypersensitivity (anaphylactic reaction, Stevens-Johnson syndrome) to saquinavir, ritonavir, or any ingredient in the formulation.1
Complete AV block without implanted pacemakers and patients at high risk of complete AV block.199
Congenital long QT syndrome.199
Refractory hypokalemia or hypomagnesemia.199 (See Cardiovascular Effects under Cautions.)
Concomitant use with drugs that increase saquinavir plasma concentrations and prolong the QT interval.199 (See Cardiovascular Effects under Cautions.)
Severe hepatic impairment.1
Concomitant use with drugs highly dependent on CYP3A for metabolism and for which elevated plasma concentrations are associated with serious and/or life-threatening events (e.g., amiodarone, cisapride, ergot alkaloids, flecainide, midazolam, propafenone, quinidine, rifampin, pimozide, triazolam).1 (See Specific Drugs and Foods under Interactions.)
Ritonavir-boosted saquinavir prolongs PR interval in a dose-dependent fashion; cases of second or third degree AV block reported rarely.199 Patients with underlying structural heart disease, preexisting conduction system abnormalities, cardiomyopathies, and ischemic heart disease may be at increased risk for developing cardiac conduction abnormalities; ECG monitoring recommended in such patients.199 Concomitant use of ritonavir-boosted saquinavir and other drugs that prolong the PR interval (e.g., calcium-channel blocking agents, β-adrenergic blockers, digoxin, atazanavir) not evaluated.199 Use ritonavir-boosted saquinavir with caution in patients receiving other drugs that prolong the PR interval, particularly drugs metabolized by CYP3A; clinical monitoring recommended.199
Ritonavir-boosted saquinavir causes dose-dependent prolongation of QT interval; torsades de pointes reported rarely.199 Perform an ECG prior to initiation of ritonavir-boosted saquinavir.199 Patients with QT interval >450 msec should not receive the drug.199 Ritonavir-boosted saquinavir may be initiated in those with baseline QT interval <450 msec; however, preform a repeat ECG after 3–4 days of therapy and discontinue the antiretroviral if QT interval is >480 msec or is prolonged >20 msecs over baseline.199 ECG monitoring recommended if ritonavir-boosted saquinavir is initiated in patients with congestive heart failure, bradyarrhythmias, hepatic impairment, and electrolyte abnormalities.199 Correct hypokalemia or hypomagnesemia prior to initiating ritonavir-boosted saquinavir; monitor these electrolytes periodically during therapy.199
Ritonavir-boosted saquinavir should not be used in conjunction with drugs that increase saquinavir plasma concentrations and prolong the QT interval.199 Manufacturer states that concomitant use of ritonavir-boosted saquinavir and drugs with the potential to increase the QT interval should be considered only when no alternative therapy is available and potential benefits outweigh risks.199 Perform an ECG prior to initiation of the drugs.199 Do not use such concomitant therapy in patients with QT interval >450 msec.199 If baseline QT interval is <450 msec, perform a repeat ECG after 3–4 days of concomitant therapy.199 If QT interval is >480 msec or is prolonged >20 msecs over baseline, clinician should use best clinical judgement regarding discontinuing ritonavir-boosted saquinavir and/or the other drug.199 Cardiology consult recommended if drug discontinuation or interruption is being considered on the basis of ECG assessment.199
Concomitant use with certain drugs not recommended (e.g., lovastatin, simvastatin, St. John’s wort, fluticasone) or require particular caution (e.g., digoxin, sildenafil, tadalafil, vardenafil).1 130 (See Specific Drugs and Foods under Interactions.)
Hyperglycemia, new-onset diabetes mellitus, or exacerbation of preexisting diabetes mellitus reported with use of PIs; diabetic ketoacidosis has occurred.1 57 129 131
Monitor blood glucose and initiate or adjust dosage of oral hypoglycemic agent or insulin as needed.1
Possibility of HIV resistant to saquinavir and possible cross-resistance to other PIs.1 Effect of saquinavir therapy on subsequent therapy with other PIs under investigation.1
Exacerbation of chronic liver dysfunction, including portal hypertension, reported in patients with hepatitis B virus (HBV) or hepatitis C virus (HCV), cirrhosis, or other underlying liver abnormalities.1
Spontaneous bleeding noted with PIs; causal relationship not established.1 57 80 127
Caution in patients with a history of hemophilia type A or B.1 80 Increased hemostatic (e.g., antihemophilic factor) therapy may be needed.1 80
During initial treatment, patients who respond to antiretroviral therapy may develop an inflammatory response to indolent or residual opportunistic infections (e.g., Mycobacterium avium complex [MAC], M. tuberculosis, cytomegalovirus [CMV], Pneumocystis jiroveci [formerly P. carinii]);1 this may necessitate further evaluation and treatment.1
Possible redistribution or accumulation of body fat, including central obesity, dorsocervical fat enlargement (“buffalo hump”), peripheral wasting, breast enlargement, and general cushingoid appearance.1 57 123 144 145 146 147 148 149 150 151
Elevated cholesterol and/or triglyceride concentrations reported.1 Markedly elevated triglyceride concentrations are a risk factor for developing pancreatitis.1
Monitor cholesterol and triglyceride concentrations prior to and periodically during ritonavir-boosted saquinavir therapy.1 Manage lipid disorders as clinically appropriate.1 (See HMG-CoA Reductase Inhibitors under Interactions.)
Each 200-mg capsule contains 63.3 mg of anhydrous lactose; this quantity should not induce specific symptoms of lactose intolerance.1
Category B.1 Antiretroviral Pregnancy Registry at 800-258-4263.1
Some experts state that based on limited pharmacokinetic data and experience with use in pregnancy, ritonavir-boosted saquinavir can be considered an alternative (not a preferred) PI for antiretroviral regimens in pregnant women.160
Not known whether distributed into human milk.1
Instruct HIV-infected women not to breast-feed because of risk of HIV transmission and risk of adverse effects in the infant.1
Safety and efficacy not established in children <16 years of age.1
Insufficient experience in those ≥65 years of age to determine whether they respond differently than younger adults.1
Use with caution because of age-related decreases in hepatic, renal, and/or cardiac function and concomitant disease and drug therapy.1
Ritonavir-boosted saquinavir not evaluated in patients with hepatic impairment; caution advised because increased saquinavir concentrations or increased hepatic enzymes may occur.1 Contraindicated in severe hepatic impairment.1
Use with caution in severe renal impairment.1
Diarrhea, abdominal discomfort, nausea, vomiting, fatigue.1 51 75
Metabolized by CYP3A.1 83 94
Substrate for p-glycoprotein.1
Inhibits CYP3A.94
Pharmacokinetic interactions likely with drugs that are inhibitors, inducers, or substrates of CYP3A with possible alteration in metabolism of saquinavir and/or other drug.1 51 83 94
Potential pharmacokinetic interaction with drugs that are inhibitors, inducers, or substrates of p-glycoprotein with possible alteration in the pharmacokinetics of saquinavir and/or other drug.1
Because dose-dependent prolongation of QT and PR intervals has been reported in individuals receiving ritonavir-boosted saquinavir, additive effects on QT and/or PR interval prolongation may occur if ritonavir-boosted saquinavir is used concomitantly with other drugs known to have similar effects.199 Concomitant use with other drugs known to prolong QT and/or PR intervals (e.g., class IA and class III antiarrhythmic agents, neuroleptics, phosphodiesterase type 5 inhibitors if used for pulmonary arterial hypertension, some antidepressants, some anti-infectives, some antihistamines) not recommended.198 199 (See Cardiovascular Effects under Cautions.)
Drug or Food | Interaction | Comments |
|---|---|---|
Antiarrhythmic agents (amiodarone, flecainide, systemic lidocaine, propafenone, quinidine) | Possible increased antiarrhythmic agent concentrations; potential for serious or life-threatening effects (e.g., cardiac arrhythmias)1 | Concomitant use with amiodarone, flecainide, propafenone, or quinidine contraindicated1 Cautious use with systemic lidocaine; monitor for toxicity and lidocaine concentrations1 |
Anticonvulsants (carbamazepine, phenobarbital, phenytoin) | Possible decreased saquinavir concentrations1 Carbamazepine: Possible increased carbamazepine concentrations with ritonavir-boosted saquinavir130 Phenytoin: Possible decreased concentrations of phenytoin and saquinavir with ritonavir-boosted saquinavir130 | Use concomitantly with caution1 Carbamazepine or phenytoin: Monitor concentrations of anticonvulsant and saquinavir and assess virologic response or consider alternative anticonvulsant130 |
Antidepressants, tricyclic | Increased amitriptyline or imipramine concentrations1 | Cautious use; monitor antidepressant concentrations1 |
Antifungals, azoles (fluconazole, itraconazole, ketoconazole, voriconazole) | Fluconazole: Possible increased saquinavir AUC;130 data not available regarding ritonavir-boosted saquinavir130 Itraconazole: Possible pharmacokinetic interaction may affect both drugs with ritonavir-boosted saquinavir 130 Ketoconazole: Increased saquinavir concentrations and AUC; no change in ketoconazole pharmacokinetics;1 possible pharmacokinetic interaction may affect both drugs with ritonavir-boosted saquinavir130 Voriconazole: Concomitant use with ritonavir-boosted saquinavir not evaluated;1 decreased voriconazole concentrations reported with low-dose ritonavir130 | Itraconazole: Appropriate dosages for concomitant use not established;1 130 decreased itraconazole dosage may be needed;130 consider monitoring itraconazole concentrations130 Ketoconazole: Appropriate dosages for concomitant use not established;1 ketoconazole dosage >200 mg daily not recommended with ritonavir-boosted saquinavir130 Voriconazole: Concomitant use of ritonavir-boosted saquinavir not recommended unless potential benefits outweigh risks;130 consider monitoring voriconazole concentrations130 |
Antimycobacterials (rifabutin, rifampin, rifapentine) | Rifabutin: Decreased saquinavir AUC (40%) with rifabutin;1 94 96 no clinically important change in saquinavir concentrations with a regimen of rifabutin 150 mg every 3 days or 300 mg every 7 days with saquinavir 400 mg twice daily and ritonavir 400 mg twice daily1 Rifampin: Decreased saquinavir AUC (80%);1 130 increased incidence of hepatotoxicity (marked increases in transaminase concentrations) with ritonavir-boosted saquinavir and rifampin1 130 173 | Rifabutin: Some clinicians recommend ritonavir-boosted saquinavir with a rifabutin dosage of 150 mg once every other day or 3 times weekly130 Rifampin: Concomitant use contraindicated1 130 173 Rifapentine: Concomitant use not recommended130 |
Atazanavir | Increased plasma concentrations of saquinavir and no change in atazanavir concentrations with saquinavir 1.6 g once daily, ritonavir 100 mg once daily, and atazanavir 300 mg once daily1 Data not available on saquinavir 1 g twice daily and ritonavir 100 mg twice daily with atazanavir 300 mg once daily1 In vitro evidence of additive antiretroviral effects175 | Appropriate dosages for concomitant use with respect to safety and efficacy not established1 130 175 |
Benzodiazepines | Alprazolam, clorazepate, diazepam, or flurazepam: Increased benzodiazepine concentrations1 130 Midazolam or triazolam: Increased benzodiazepine concentrations;1 130 potential for prolonged or increased sedation or respiratory depression1 Lorazepam, oxazepam, temazepam: No data, but may have less potential for pharmacokinetic interaction with PIs compared with other benzodiazepines130 | Clinical importance of interaction with alprazolam, clorazepate, diazepam, or flurazepam unknown;1 decreased benzodiazepine dosage may be needed;1 consider using a benzodiazepine with less potential for pharmacokinetic interaction (lorazepam, oxazepam, temazepam)130 Manufacturer of saquinavir states that concomitant use with midazolam or triazolam contraindicated;1 however, some experts state a single parenteral dose of midazolam can be used with caution in a monitored situation for procedural sedation130 |
Calcium-channel blocking agents | Possible increased concentrations of the calcium-channel blocking agent (e.g., amlodipine, diltiazem, felodipine, isradipine, nicardipine, nifedipine, nimodipine, verapamil, nisoldipine)1 130 | Use concomitantly with caution;1 130 monitor for toxicity;1 130 adjust dosage of calcium-channel blocking agent based on clinical response and toxicities130 |
Cisapride | Pharmacokinetic interaction; potential for serious or life-threatening reactions (e.g., cardiac arrhythmias)1 | Concomitant use contraindicated1 130 |
Corticosteroids (dexamethasone, fluticasone) | Fluticasone nasal spray/oral inhalation: Increased fluticasone concentrations with ritonavir-boosted saquinavir resulting in decreased cortisol concentrations1 Dexamethasone: Possible decreased saquinavir concentrations;1 130 concomitant use with ritonavir-boosted saquinavir not studied1 | Fluticasone nasal spray/oral inhalation: Concomitant use not recommended unless potential benefits outweigh risk of systemic corticosteroid adverse effects1 130 Dexamethasone: Use concomitantly with caution; saquinavir may be less effective1 |
Dapsone | Possible increased dapsone concentrations1 | Use with caution1 |
Darunavir | Decreased concentrations of darunavir and no effect on saquinavir concentrations with darunavir 400 mg, ritonavir 100 mg, and saquinavir 1 g twice daily193 | Concomitant use of ritonavir-boosted darunavir and saquinavir not recommended130 193 |
Delavirdine | Increased saquinavir AUC;1 140 130 no effect on delavirdine concentrations130 Concomitant use with ritonavir-boosted saquinavir not evaluated1 | Manufacturer of saquinavir states appropriate dosages for concomitant use with respect to safety and efficacy not established1 Some clinicians recommend using saquinavir 1 g twice daily and ritonavir 100 mg twice daily with usual dosage of delavirdine130 |
Didanosine | In vitro evidence of additive or synergistic antiretroviral effects1 2 14 29 30 47 69 | |
Digoxin | Ritonavir-boosted saquinavir: Increased digoxin concentrations1 | Caution advised; monitor digoxin concentrations; may need to reduce the digoxin dose1 |
Efavirenz | Decreased peak plasma concentrations and AUC of saquinavir;130 153 decreased efavirenz concentrations130 Concomitant use with ritonavir-boosted saquinavir not evaluated1 In vitro evidence of synergistic antiretroviral effects1 | Manufacturer of saquinavir states appropriate dosages for concomitant use with respect to safety and efficacy not established1 Some clinicians recommend using saquinavir 1 g twice daily and ritonavir 100 mg twice daily with usual dosage of efavirenz130 |
Emtricitabine | In vitro evidence of additive or synergistic antiretroviral effectsa | |
Enfuvirtide | Pharmacokinetic interaction unlikely1 | |
Ergot alkaloids (dihydroergotamine, ergonovine, ergotamine, methylergonovine) | Possibility of pharmacokinetic interaction; potential for serious or life-threatening reactions (e.g., acute ergot toxicity)1 | Concomitant use contraindicated1 130 If treatment of uterine atony and excessive postpartum bleeding is indicated in a woman receiving saquinavir, use methylergonovine maleate (Methergine) only if alternative treatments cannot be used and if potential benefits outweigh risks; use methylergonovine at lowest dosage and shortest duration possible160 |
Estrogens/Progestins | Hormonal contraceptives: Possible decreased ethinyl estradiol concentrations1 | Alternative or additional contraceptive measures should be used when estrogen-based oral contraceptive is used concomitantly with ritonavir-boosted saquinavir1 |
Etravirine | Ritonavir-boosted saquinavir (saquinavir 1 g twice daily and ritonavir 100 mg twice daily): Decrease in AUC (33%) of etravirine; no change in plasma concentrations of saquinavir130 196 No in vitro evidence of antagonistic antiretroviral effects196 | Dosage adjustment not needed130 196 Decrease in systemic exposure to etravirine similar to that in patients receiving etravirine in conjunction with ritonavir-boosted darunavir (a combination found to be safe and effective)130 196 |
Fosamprenavir | Appropriate dosages for concomitant use with respect to safety and efficacy not established130 | |
Garlic | Decreased saquinavir plasma concentrations and AUC with garlic supplements.1 61 Data not available on concomitant use with ritonavir-boosted saquinavir1 | Avoid garlic supplements1 61 130 |
Grapefruit juice | Oral bioavailability of saquinavir increased103 | |
Histamine H2-receptor antagonists (ranitidine) | Ranitidine: Increased concentrations of saquinavir1 Data not available on concomitant use with ritonavir-boosted saquinavir1 | Appropriate dosages for concomitant use with respect to safety and efficacy not established1 |
HMG-CoA reductase inhibitors | Decreased clearance and increased concentrations of some HMG-CoA reductase inhibitors (e.g., atorvastatin, lovastatin, rosuvastatin, simvastatin) with potential for increased risk of myopathy (including rhabdomyolysis)1 130 Decreased concentrations of pravastatin with ritonavir-boosted saquinavir130 | Concomitant use with lovastatin or simvastatin not recommended1 95 130 Caution if used with other HMG-CoA reductase inhibitors metabolized by the CYP3A4 pathway (e.g., atorvastatin)1 95 130 If used with atorvastatin or rosuvastatin, use lowest possible dosage of the HMG-CoA reductase inhibitor1 130 Consider using HMG-CoA reductase inhibitors with a low potential for interaction (e.g., fluvastatin)1 130 |
Immunosuppressive agents (cyclosporine, sirolimus, tacrolimus) | Increased immunosuppressant concentrations1 155 | Monitor immunosuppressive agent concentrations1 |
Indinavir | Increased saquinavir concentrations1 Data not available on concomitant use with ritonavir-boosted saquinavir1 | Appropriate dosages for concomitant use with respect to safety and efficacy not established 1 130 |
Lamivudine | In vitro evidence of additive or synergistic antiretroviral effects1 2 14 29 30 47 69 |
|
Lopinavir | Saquinavir concentrations achieved with a regimen of saquinavir 1 g twice daily with 400 mg of lopinavir and 100 mg of ritonavir twice daily similar to those with saquinavir 1 g twice daily and ritonavir 100 mg twice daily1 189 | Recommended dosage is saquinavir 1 g twice daily with 400 mg of lopinavir and 100 mg of ritonavir twice daily1 130 169 |
Macrolides (clarithromycin) | Increased saquinavir and clarithromycin AUC; decreased 14-hydroxyclarithromycin AUC1 130 | Manufacturer of saquinavir states appropriate dosages for concomitant use with respect to safety and efficacy not established;1 monitor for clarithromycin toxicities;130 in patients receiving ritonavir-boosted saquinavir, consider reducing clarithromycin dosage by 50% in those with Clcr 30–60 mL/minute and by 75% in those with Clcr <30 mL/minute; dosage adjustment not needed in those with normal renal function 1 130 |
Maraviroc | Ritonavir-boosted saquinavir: Substantially increased maraviroc concentrations130 195 | Ritonavir-boosted saquinavir: Recommended dosage of maraviroc is 150 mg twice daily130 195 |
Methadone | Decreased methadone concentrations with ritonavir-boosted saquinavir1 130 | Monitor closely and consider that increased methadone dosage may be needed1 130 |
Nelfinavir | Increased saquinavir concentrations and increased nelfinavir concentrations1 123 Data not available on concomitant use with ritonavir-boosted saquinavir1 123 | Manufacturer of nelfinavir states appropriate dosages for concomitant use with respect to safety and efficacy not established123 Saquinavir 1.2 g twice daily with nelfinavir 1.25 g twice daily results in adequate plasma concentrations of both PIs1 |
Nevirapine | Decreased saquinavir concentrations; no change in nevirapine pharmacokinetics1 102 130 Concomitant use with ritonavir-boosted saquinavir not evaluated1 In vitro evidence of additive or synergistic antiretroviral effects1 | Manufacturer of saquinavir states appropriate dosages for concomitant use with respect to safety and efficacy not established 1 Consider saquinavir 1 g twice daily with ritonavir 100 mg twice daily with usual nevirapine dosage130 |
Pimozide | Pharmacokinetic interaction; potential for serious or life-threatening reactions (e.g., cardiac arrhythmias)1 | Concomitant use contraindicated1 130 |
Proton-pump inhibitors | Omeprazole with ritonavir-boosted saquinavir: Increased concentrations of saquinavir1 | Caution advised if ritonavir-boosted saquinavir used with a proton-pump inhibitor;1 monitor for saquinavir toxicities (GI symptoms, increased triglycerides, deep vein thrombosis)1 130 |
Ritonavir | Increased saquinavir concentrations (increased 1124% with saquinavir 1 g twice daily and ritonavir 100 mg twice daily compared with saquinavir 600 mg 3 times daily);1 130 no change in ritonavir concentrations130 Concomitant low-dose ritonavir used to therapeutic advantage (ritonavir-boosted saquinavir)1 130 Ritonavir-boosted saquinavir has produced dose-dependent prolongation of QT and PR intervals198 199 | Recommended dosage is saquinavir 1 g twice daily with ritonavir 100 mg twice daily1 130 |
St. John’s wort (Hypericum perforatum) | Possible decreased saquinavir concentrations1 59 162 163 | Concomitant use contraindicated1 130 |
Sildenafil | Increased sildenafil concentrations and increased risk of sildenafil-associated adverse effects (e.g., hypotension, visual changes, prolonged erection)1 130 154 | Sildenafil for treatment of erectile dysfunction: Use caution and reduced initial sildenafil dosage of 25 mg dose and do not exceed 25 mg every 48 hours); closely monitor for adverse effects1 130 154 Sildenafil for treatment of pulmonary arterial hypertension (PAH): Concomitant use contraindicated130 |
Stavudine | In vitro evidence of additive or synergistic antiretroviral effects1 2 14 29 30 47 69 |
|
Tadalafil | Possible increased tadalafil concentrations and increased risk of tadalafil-associated adverse effects (e.g., hypotension, visual changes, prolonged erection)1 130 | Use initial tadalafil dosage of 5 mg; do not exceed a single dose of 10 mg in 72 hours; monitor closely for adverse effects1 130 |
Tenofovir | No clinically important change in saquinavir concentrations with saquinavir 1 g twice daily and ritonavir 100 mg twice daily with tenofovir 300 mg once daily1 192 | Dosage adjustment not needed with ritonavir-boosted saquinavir192 |
Tipranavir | Decreased saquinavir concentrations1 | Concomitant use not recommended;1 130 appropriate dosage not established130 |
Trazodone | Possible increased trazodone concentrations; increased risk of trazodone-associated adverse effects1 | Caution; decreased trazodone dosage may be needed1 |
Vardenafil | Possible increased vardenafil concentrations and increased risk of vardenafil-associated adverse effects (e.g., hypotension, visual changes, prolonged erection)1 130 | Do not exceed a single vardenafil dose of 2.5 mg in 72 hours; monitor closely for adverse effects1 130 |
Warfarin | Possible altered warfarin concentrations1 | Monitor INR1 |
Zidovudine | In vitro evidence of additive or synergistic antiretroviral effects1 2 14 29 30 47 69 |
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Saquinavir mesylate incompletely absorbed from GI tract;1 44 48 49 50 51 oral bioavailability is low (calculated bioavailability 4%).1 3 44 48 49 50 51
When saquinavir used with low-dose ritonavir, there is a 5-fold increase in mean AUC of saquinavir, increases of a similar magnitude in trough and peak plasma concentrations, and less interindividual variability in saquinavir pharmacokinetics compared with saquinavir without ritonavir.185 186
Presence of food in GI tract substantially increases absorption of saquinavir.1
Effect of food on ritonavir-boosted saquinavir not evaluated.1
Not fully characterized.1
Not known whether saquinavir crosses the placenta or is distributed into milk.1 64
Negligible concentrations detected in CSF.1 64 157
98%.1
Metabolized by CYP3A.1 51
Excreted principally in feces as unabsorbed drug and metabolites.1
3–6.8 hours.184 185
25°C (may be exposed to 15–30°C).1
25°C (may be exposed to 15–30°C).1
Pharmacologically related to other PIs (e.g., atazanavir, fosamprenavir, indinavir, lopinavir, nelfinavir, ritonavir); differs structurally from these drugs and also differs pharmacologically and structurally from other currently available antiretrovirals.1 2 6 8 10
