Inderal
Inderal Medication Information:
Inderal medication comes in several different strengths; click on the strength you need to view prices from pharmacies competing to earn your business.
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Inderal 10 mg
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Inderal LA 60 mg
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Inderal LA 80 mg
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Inderal LA 120 mg
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Inderal LA 160 mg
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Pharmacology
Pharmacokinetics
Propranolol from Inderal-LA capsules is almost completely absorbed from the gastrointestinal tract. A large part of the absorbed drug is lost from the systemic circulation due to first-pass metabolism in the liver. The first-pass metabolism is saturable. Steady-state plasma propranolol concentrations from Inderal-LA are proportional to the dose over the range of 60 to 160 mg/day although there is considerable intersubject variation. In healthy volunteers steady state was achieved after 2 or 3 days administration of Inderal-LA.
Peak blood levels following administration of Inderal-LA capsules occur at about 6 hours and the apparent plasma half-life has been reported to be between 10 and 12 hours i.e. 2 to 3 times that of the conventional tablet formulation.
When measured at steady state over a 24-hour period the areas under the propranolol plasma concentration-time curve (AUCs) for the LA-capsules are approximately 60 to 65% of the AUCs for a comparable divided daily dose of propranolol tablets. The lower AUCs for the Inderal-LA capsules are due to greater hepatic metabolism of propranolol because of slower absorption. Over a 24-hour period, blood levels are fairly constant for about 12 hours, then decline exponentially.
Indications
Inderal-LA (propranolol hydrochloride) extended release capsules are indicated for maintenance therapy in the treatment of hypertension and prophylaxis of angina pectoris.
As for Inderal, the combination of Inderal-LA with thiazide-like diuretics and/or peripheral vasodilators has been shown to be compatible and generally more effective than Inderal-LA alone. Experience with most commonly used antihypertensive agents has not suggested evidence of incompatibility.
Treatment must always be initiated and individual titration of dosage carried out using the conventional tablets. The long-acting formulation may be used for maintenance provided the dosage requirement is suitable.
Inderal-LA is not indicated for the emergency treatment of hypertensive crises.
Precautions
There may be increased difficulty in treating an allergic type reaction in patients on beta-blockers. In these patients, the reaction may be more severe due to pharmacological effects of beta-blockers and problems with fluid changes. Epinephrine should be administered with caution since it may not have its usual effects in the treatment of anaphylaxis. On the one hand, larger doses of epinephrine may be needed to overcome the bronchospasm, while on the other, these doses can be associated with excessive alpha adrenergic stimulation with consequent hypertension, reflex bradycardia and heart-block and possible potentiation of bronchospasm. Alternatives to the use of large doses of epinephrine include vigorous supportive care such as fluids, and the use of beta agonists including parenteral salbutamol or isoproterenol to overcome bronchospasm, and norepinephrine to overcome hypotension.
Some slowing of heart due to unopposed vagal activity is usual in patients receiving propranolol; however, occasionally severe bradycardia occurs and may lead to vertigo, syncopal attacks or orthostatic hypotension. Patients, especially those with limited cardiac reserve should be monitored for signs of excessive bradycardia. Should the patient become symptomatic the dose of propranolol should be decreased or, if necessary, the drug should be discontinued. If it is essential to correct the bradycardia i.v. atropine or isoproterenol should be considered.
It has been reported that administration of propranolol to control cardiac arrhythmias in acute myocardial infarction has caused marked reduction in cardiac output. Therefore, the doses of propranolol should be kept to the minimum in patients with severe myocardial infarction. Caution should be exercised when administering propranolol in such situations, especially when a large portion of the myocardium has been damaged due to coronary occlusion since adequate sympathetic drive should be preserved to maintain ventricular function. Prior administration of other antiarrhythmic cardiac depressant drugs, such as procainamide or quinidine may potentiate the cardiac depressant activity of propranolol. Prior digitalization may be indicated and atropine should be at hand to control bradycardia.
The combination of propranolol with a thiazide like diuretic and/or peripheral vasodilator produces a greater fall in blood pressure than either drug alone. This occurs regardless of which drug is administered first. The same degree of blood pressure control can be achieved by lower than usual dosages of each drug. Therefore, when using such combined therapy, careful monitoring of the dosages is required until the patient is stabilized.
Patients receiving catecholamine depleting drugs such as reserpine or guanethidine should be closely observed if propranolol is administered concomitantly. The added catecholamine blocking action of this drug may produce an excessive reduction of the resting sympathetic nervous activity.
In patients on long-term treatment with propranolol, laboratory determinations should be made at regular intervals. The drug should be used with caution in patients with impaired renal and hepatic functions.
Supplied
60 mg
Each white/light blue, extended-release capsule, identified by 3 narrow bands, 1 wide band, and INDERAL-LA 60, contains: propranolol HCl 60 mg. Nonmedicinal ingredients: ethylcellulose, hydroxypropyl methylcellulose and microcrystalline cellulose; empty capsule: FD&C Blue No. 1, FD&C Red No. 3, gelatin, silicon dioxide, sodium lauryl sulfate and titanium dioxide. Energy: 0.84 kJ (0.2 kcal). Alcohol-, gluten-, lactose-, sodium-, sugar-, sulfites- and tartrazine-free. Bottles of 100.
80 mg
Each light blue, extended-release capsule, identified by 3 narrow bands, 1 wide band, and INDERAL-LA 80, contains: propranolol HCl 80 mg. Nonmedicinal ingredients: ethylcellulose, hydroxypropyl methylcellulose and microcrystalline cellulose; empty capsule: FD&C Blue No. 1, FD&C Red No. 3, gelatin, silicon dioxide, sodium lauryl sulfate and titanium dioxide. Alcohol-, gluten-, lactose-, sodium-, sugar-, sulfites- and tartrazine-free. Energy: 0.84 kJ (0.2 kcal). Bottles 100.
160 mg
Each dark blue, extended-release capsule, identified by 3 narrow bands, 1 wide band, and INDERAL-LA 160, contains: propranolol HCl 160 mg. Nonmedicinal ingredients: ethylcellulose, hydroxypropyl methylcellulose and microcrystalline cellulose; empty capsule: FD&C Blue No. 1, gelatin and titanium dioxide. Energy: 1.26 kJ (0.3 kcal). Alcohol-, gluten-, lactose-, sodium-, sugar-, sulfites- and tartrazine-free. Bottles of 100 and 500.
120 mg
Each light blue/dark blue, extended-release capsule, identified by 3 narrow bands, 1 wide band and INDERAL-LA 120, contains: propranolol HCl 120 mg. Nonmedicinal ingredients: ethylcellulose, hydroxypropyl methylcellulose and microcrystalline cellulose; empty capsule: FD&C Blue No. 1, FD&C Red No. 3, gelatin, silicon dioxide, sodium lauryl sulfate and titanium dioxide. Energy: 0.84 kJ (0.2 kcal). Alcohol-, gluten-, lactose-, sodium-, sugar-, sulfites- and tartrazine-free. Bottles of 100.
Contraindications
Bronchospasm, including bronchial asthma; allergic rhinitis during the pollen season; sinus bradycardia and greater than first degree block; cardiogenic shock; right ventricular failure secondary to pulmonary hypertension; congestive heart failure (see Warnings) unless the failure is secondary to a tachyarrhythmia treatable with propranolol.
Warnings
Lactation
Propranolol is excreted in human milk. Caution should be exercised when propranolol is administered to a nursing woman.
Children
While experience with propranolol in children under 12 is limited, the indications for which this drug is recommended occur infrequently in childhood. Although reports fail to indicate that children respond in a manner different from the adult, physicians are advised to undertake treatment with caution.
Pregnancy
Pregnancy and Fetal Injury: Propranolol can cause fetal harm when administered to a pregnant woman. The safe use of propranolol in pregnancy has not been established. Use of any drug in pregnancy or in women of childbearing potential requires that the possible risk to mother and/or fetus be weighed against the expected therapeutic benefit. Post-marketing case reports including perinatal complications, such as small placentas, intrauterine growth retardation and congenital abnormalities have been reported in neonates where the mother took propranolol during pregnancy. Some infants born to mothers treated with propranolol were reported to have hypoglycemia, bradycardia and/or respiratory depression. Adequate facilities for monitoring such infants at birth should be available. Propranolol should be used in pregnancy only if the potential benefit justifies the potential risk to the fetus.
Adverse Effects
Gastrointestinal
nausea, vomiting, epigastric distress, anorexia, bloating, mild diarrhea, constipation.
Central Nervous System
dizziness, lethargy, weakness, drowsiness, headache, insomnia, fatigue, anorexia, anxiety, mental depression, poor concentration, reversible amnesia and catatonia, vivid dreams with or without insomnia, hallucinations, paresthesia, incoordination.
Others
reduction or loss of libido; reversible alopecia and rarely: diminution and loss of hearing; tinnitus; visual disturbances; diminished vision, conjunctivitis; thrombocytopenic purpura; pharyngitis and agranulocytosis, fever combined with aching and sore throat; flushing of the face.
Respiratory
bronchospasm; laryngospasm and respiratory distress (see Contraindications and Warnings).
Dermatologic
A few cases of erythematous rashes and increase of facial acneiform lesions have been reported; urticaria; exfoliative psoriasiform eruption, Stevens-Johnson syndrome, toxic epidermal necrolysis, exfoliative dermatitis and erythema multiforme.
Clinical Laboratory Test Findings
Elevated blood urea levels in patients with severe heart disease, elevated serum transaminase, alkaline phosphatase, and lactate dehydrogenase have been reported.
Allergic
hypersensitivity reactions, including anaphylactic/anaphylactoid reactions.
Cardiovascular
congestive heart failure (see Warnings); secondary effects of decreased cardiac output which could include: syncope, vertigo, lightheadedness, decreased renal perfusion and rarely, postural hypotension; intensification of AV block and hypotension; severe bradycardia; claudication and cold extremities, Raynaud's phenomenon; dyspnea; palpitations; precordial pain.
Overdose
Symptoms
Several reports in the published literature describe cases in which propranolol was used as a suicide agent. In most cases, other agents, e.g., alcohol, have also been involved. One patient who died was thought to have ingested 3600 mg of propranolol. Survival of patients taking higher single doses has, however, also been reported. The common signs to be expected in overdosage are bradycardia, hypotension, bronchospasm, or acute cardiac failure.
Treatment
If overdosage occurs, in all cases therapy with propranolol should be discontinued and the patient observed closely. In addition the following therapeutic measures are suggested:
Bradycardia: Administer atropine incrementally in 600 µg (0.6 mg) doses. If there is no response to vagal blockade, administer isoproterenol cautiously.
Cardiac Failure: Digitalization and diuretics.
Hypotension: Vasopressors, e.g., epinephrine or levarterenol. (There is evidence that epinephrine is the drug of choice.)
Bronchospasm: Administer isoproterenol and aminophylline.
Dosage
Inderal-LA Extended-Release Capsules are intended for maintenance therapy in those patients requiring doses within the range of 60 to 320 mg/day. Initiation of treatment and individual titration of dosage should be carried out using the conventional tablets. Inderal-LA may be preferred for maintenance because of the convenience of once-daily dosage. Patients with angina or hypertension on a maintenance regimen within the range of 60 to 320 mg/day regular tablets taken in divided doses may be changed to the appropriate number of Inderal-LA capsules taken once daily in the morning or evening.
However, Inderal-LA should not be considered a simple mg-for-mg substitute for conventional propranolol tablets and blood levels achieved are lower than those of 2 to 4 times daily dosing with the same dose. When changing to Inderal-LA from conventional propranolol tablets, a possible need for retitration upwards should be considered, especially to maintain effectiveness at the end of the dosing interval. In most clinical settings, however, such as hypertension or angina where there is little correlation between plasma levels and clinical effect, Inderal-LA has been shown to be therapeutically equivalent to the same mg dose of conventional propranolol as assessed by 24-hour effects on blood pressure, and on 24-hour exercise responses of heart rate, systolic pressure, and rate pressure product. Inderal-LA can provide effective beta blockade for 24-hour periods.
When propranolol is combined with another antihypertensive agent which is already being administered, therapy should be initiated with conventional propranolol tablets following usual dosage recommendations. Once adequate blood pressure control has been obtained, Inderal-LA capsules may be used for maintenance provided the dosage requirement is suitable.
In the treatment of hypertension, if required, further reduction of blood pressure may be attained by the addition of diuretic and/or peripheral vasodilator. Addition of another antihypertensive agent should, however, be gradual, beginning with 50% of the usual recommended starting dose, to avoid excessive reduction of blood pressure.
