Apsolol - General Information
A widely used non-cardioselective beta-adrenergic antagonist. Apsolol is used in the treatment or prevention of many disorders including acute myocardial infarction, arrhythmias, angina pectoris, hypertension, hypertensive emergencies, hyperthyroidism, migraine, pheochromocytoma, menopause, and anxiety.
Pharmacology of Apsolol
Apsolol, the prototype of the beta-adrenergic receptor antagonists, is a competitive, nonselective beta-blocker similar to nadolol without intrinsic sympathomimetic activity. Propanolol is a racemic compound; the l-isomer is responsible for adrenergic blocking activity.
Apsolol for patients
PROPRANOLOL - ORAL
IMPORTANT NOTE: The following information is intended to supplement, not substitute for, the expertise and judgment of your
physician, pharmacist or other healthcare professional. It should not be construed to indicate that use of the drug is safe,
appropriate, or effective for you. Consult your healthcare professional before using this drug.
PROPRANOLOL - ORAL
COMMON BRAND NAME(S): Inderal
WARNING: If you have chest pain (angina) or heart disease (e.g., coronary artery disease, ischemic heart disease, high blood
pressure), do not stop using this drug without first consulting your doctor. Your condition may become worse when the drug is
suddenly stopped. If your doctor decides you should no longer use this drug, you must gradually decrease your dose according
to your doctor's instructions.
When gradually stopping this medication, it is recommended that you temporarily limit physical activity to decrease strain on
the heart. Seek immediate medical attention if you develop: worsening chest pain, tightness or pressure in the chest, chest pain
spreading to the jaw/neck/arm, sweating, trouble breathing or fast/irregular heartbeat.
This medication is a beta-blocker used to treat chest pain (angina), high blood pressure, irregular heartbeats, migraine headaches,
tremors, and other conditions as determined by your doctor. It is also used after an acute heart attack to improve survival.
Lowering high blood pressure helps prevent strokes, heart attacks and kidney problems.
This drug works by blocking the action of certain natural chemicals in your body (such as epinephrine) that affect the heart and
blood vessels. This results in a lowering of heart rate, blood pressure, and strain on the heart.
This medication has also been used for anxiety.
HOW TO USE:
Take this medication by mouth, as directed by your doctor. Use this medication regularly in order to get the most benefit from it.
Remember to use it at the same time(s) each day.
This drug is not effective if you use it only when chest pain or a migraine headache occurs. It is very important to take this
medication regularly as prescribed to help prevent these conditions.
The dosage is based on your medical condition and response to therapy. It may take 1 or 2 weeks before the full benefit of this
drug takes effect. It is important to continue taking this medication even if you feel well. Most people with high blood pressure
do not feel sick.
Do not suddenly stop taking this medication without consulting your doctor. Your condition may become worse when the drug is suddenly
stopped. Refer to the Warning section.
You may experience dizziness, lightheadedness, drowsiness, tiredness, diarrhea, unusual dreams, trouble sleeping, or vision problems
as your body adjusts to the medication. If any of these effects persist or worsen, notify your doctor or pharmacist promptly.
This drug may reduce blood flow to your hands and feet, causing them to feel cold. Smoking may worsen this effect. Dress warmly and
avoid tobacco use.
Tell your doctor immediately if any of these unlikely but serious side effects occur: symptoms of a very slow heartbeat (e.g.,
persistent dizziness, fainting, unusual fatigue), bluish discoloration of the fingers and toes, numbness/tingling/swelling of the
hands or feet, decreased sexual ability, reversible hair loss, mental/mood changes, trouble breathing, cough, unexplained or sudden
weight gain, increased thirst, increased urination.
Tell your doctor immediately if any of these highly unlikely but very serious side effects occur: easy bruising or bleeding, persistent
sore throat or fever.
In the unlikely event you have a serious allergic reaction to this drug, seek medical attention immediately. Symptoms of a serious
allergic reaction include: rash, itching, swelling, severe dizziness, trouble breathing.
If you notice other effects not listed above, contact your doctor or pharmacist.
Before taking propranolol, tell your doctor or pharmacist if you are allergic to it; or if you have any other allergies.
This medication should not be used if you have certain medical conditions. Before using this medicine, consult your doctor or
pharmacist if you have: certain types of irregular heartbeats (e.g., sinus bradycardia, second or third degree atrioventricular block),
cardiogenic shock, severe heart failure (overt or decompensated type), asthma, a certain type of tumor (untreated pheochromocytoma).
Before using this medication, tell your doctor or pharmacist your medical history, especially of: heart failure (treated, compensated
type), other breathing problems (e.g., chronic obstructive lung disease), diabetes, overactive thyroid disease (hyperthyroidism),
kidney disease, liver disease, blood circulation problems (e.g., Raynaud's disease), skin conditions (e.g., psoriasis), mental/mood
disorders (e.g., depression), certain muscle disease (myasthenia gravis).
Before having surgery, tell your doctor or dentist that you are taking this medication.
If you have diabetes, this medication may mask the fast/pounding heartbeat you would usually feel when your blood sugar level falls
too low (hypoglycemia). Other symptoms of a low blood sugar level such as dizziness or sweating are unaffected by this drug.
This drug may make you dizzy or drowsy; use caution engaging in activities requiring alertness such as driving or using machinery.
Limit alcoholic beverages.
To minimize dizziness and lightheadedness, get up slowly when rising from a seated or lying position.
This drug should be used only when clearly needed during pregnancy. Discuss the risks (e.g., low birth weight) and benefits with your
This drug passes into breast milk. Consult your doctor before breast-feeding.
This drug should not be used with the following medications because very serious interactions may occur: mibefradil, certain psychiatric
drugs (phenothiazines such as chlorpromazine, thioridazine).
If you are currently using any of these medications, tell your doctor or pharmacist before starting this drug.
Before using this medication, tell your doctor or pharmacist of all prescription and nonprescription products you may use, especially
of: alpha-blockers (e.g., prazosin), certain antacids (aluminum hydroxide gel), anti-depressant drugs (e.g., amitriptyline, fluoxetine,
paroxetine), anti-diabetic drugs (e.g., glipizide, glyburide, insulin), barbiturates (e.g., phenobarbital), calcium channel blockers
(e.g., diltiazem, verapamil), cimetidine, epinephrine, ergotamine-like drugs, general anesthesia, haloperidol, other heart drugs (e.g.,
amiodarone, digoxin, propafenone, quinidine, intravenous lidocaine), other drugs to treat high blood pressure (e.g., clonidine,
hydralazine, methyldopa, reserpine), medications for overactive thyroid disease (e.g., methimazole, propylthiouracil), neuromuscular
blocking drugs, non-steroidal anti-inflammatory drugs (e.g., indomethacin, ibuprofen), phenytoin, rifamycins (e.g., rifampin),
rizatriptan, St. John's wort, theophylline.
Check the labels on all your medicines (e.g., cough-and-cold products, diet aids) because they may contain ingredients that could
increase your heart rate or blood pressure. Ask your pharmacist about the safe use of those products.
This product can affect the results of certain lab tests. Make sure laboratory personnel and your doctors know you use this drug.
Do not start or stop any medicine without doctor or pharmacist approval.
If overdose is suspected, contact your local poison control center or emergency room immediately. US residents can call the US national
poison hotline at 1-800-222-1222. Canadian residents should call their local poison control center directly. Symptoms of overdose may
include unusually slow heartbeat, severe dizziness, slow or shallow breathing, weakness, or fainting.
Do not share this medication with others. Lifestyle changes such as stress reduction programs, exercise and dietary changes may increase
the effectiveness of this medicine. Talk to your doctor or pharmacist about lifestyle changes that might benefit you.
Have your blood pressure and pulse checked regularly while taking this medication. It may be best to learn how to monitor your own blood
pressure and pulse. Discuss this with your doctor.
If you miss a dose, take it as soon as you remember, but not if it is within 4 hours of the next dose. If it is within 4 hours of the
next dose, skip the missed dose and resume your usual dosing schedule. Do not double the dose to catch up.
Store at room temperature between 68-77 degrees F (20-25 degrees C) away from light and moisture. Do not store in the bathroom. Keep
all medicines away from children and pets.
Patients receiving catecholamine-depleting drugs such as reserpine should be closely observed if Propranolol HCl is administered. The added catecholamine-blocking action may produce an excessive reduction of resting sympathetic nervous activity, which may result in hypotension, marked bradycardia, vertigo, syncopal attacks, or orthostatic hypotension.
Caution should be exercised when patients receiving a beta blocker are administered a calcium-channel blocking drug, especially intravenous verapamil, for both agents may depress myocardial contractility or atrioventricular conduction. On rare occasions, the concomitant intravenous use of a beta blocker and verapamil has resulted in serious adverse reactions, especially in patients with severe cardiomyopathy, congestive heart failure, or recent myocardial infarction.
Blunting of the antihypertensive effect of beta-adrenoceptor blocking agents by nonsteroidal anti-inflammatory drugs has been reported.
Hypotension and cardiac arrest have been reported with the concomitant use of propranolol and haloperidol.
Aluminum hydroxide gel: Greatly reduces intestinal absorption of propranolol.
Ethanol: Slows the rate of absorption of propranolol.
Phenytoin, phenobarbitone: and rifampin accelerate propranolol clearance.
Chlorpromazine: When used concomitantly with propranolol, results in increased plasma levels of both drugs.
Antipyrine: and lidocaine have reduced clearance when used concomitantly with propranolol.
Thyroxine: May result in a lower than expected T3 concentration when used concomitantly with propranolol.
Cimetidine Decreases the hepatic metabolism of propranolol, delaying elimination and incre:asing blood levels.
Theophylline: Clearance is reduced when used concomitantly with propranolol.
Propranolol HCl is contraindicated in 1) cardiogenic shock, 2) sinus bradycardia and greater than first degree block, 3) bronchial asthma, 4) congestive heart failure unless the failure is secondary to a tachyarrhythmia treatable with Propranolol HCl.
Additional information about Apsolol
Apsolol Indication: For the prophylaxis of migraine.
Mechanism Of Action: Like atenolol and metoprolol, propranolol competes with sympathomimetic neurotransmitters such as catecholamines for binding at beta(1)-adrenergic receptors in the heart and vascular smooth muscle, inhibiting sympathetic stimulation. This results in a reduction in resting heart rate, cardiac output, systolic and diastolic blood pressure, and reflex orthostatic hypotension. Higher doses of atenolol also competitively block beta(2)-adrenergic responses in the bronchial and vascular smooth muscles.
Drug Interactions: Acetohexamide The beta-blocker decreases the symptoms of hypoglycemia
Chlorpropamide The beta-blocker decreases the symptoms of hypoglycemia
Cimetidine Cimetidine increases the effect of the beta-blocker
Clonidine Increased hypertension when clonidine stopped
Disopyramide The beta-blocker increases toxicity of disopyramide
Gliclazide The beta-blocker decreases the symptoms of hypoglycemia
Glipizide The beta-blocker decreases the symptoms of hypoglycemia
Glisoxepide The beta-blocker decreases the symptoms of hypoglycemia
Glibenclamide The beta-blocker decreases the symptoms of hypoglycemia
Glycodiazine The beta-blocker decreases the symptoms of hypoglycemia
Insulin The beta-blocker decreases the symptoms of hypoglycemia
Lidocaine The beta-blocker increases the effect and toxicity of lidocaine
Maprotiline Apsolol increases the serum levels of cisapride
Methyldopa Possible hypertensive crisis
Repaglinide The beta-blocker decreases the symptoms of hypoglycemia
Propafenone Propafenone increases the effect of the beta-blocker
Rifampin Rifampin decreases the effect of the metabolized beta-blocker
Rizatriptan Apsolol increases the effect and toxicity of rizatriptan
Tolazamide The beta-blocker decreases the symptoms of hypoglycemia
Tolbutamide The beta-blocker decreases the symptoms of hypoglycemia
Verapamil Increased effect of both drugs
Prazosin Risk of hypotension at the beginning of therapy
Haloperidol Increased effect of both drugs
Hydralazine Increased effect of both drugs
Epinephrine Hypertension, then bradycardia
Diltiazem Increased risk of bradycardia
Chlorpromazine Increased effect of both drugs
Aminophylline Antagonism of action and increased effect of theophylline
Dyphylline Antagonism of action and increased effect of theophylline
Oxtriphylline Antagonism of action and increased effect of theophylline
Theophylline Antagonism of action and increased effect of theophylline
Amobarbital The barbiturate decreases the effect of metabolized beta-blocker
Aprobarbital The barbiturate decreases the effect of metabolized beta-blocker
Butabarbital The barbiturate decreases the effect of metabolized beta-blocker
Butalbital The barbiturate decreases the effect of metabolized beta-blocker
Butethal The barbiturate decreases the effect of metabolized beta-blocker
Dihydroquinidine barbiturate The barbiturate decreases the effect of metabolized beta-blocker
Heptabarbital The barbiturate decreases the effect of metabolized beta-blocker
Hexobarbital The barbiturate decreases the effect of metabolized beta-blocker
Methohexital The barbiturate decreases the effect of metabolized beta-blocker
Methylphenobarbital The barbiturate decreases the effect of metabolized beta-blocker
Pentobarbital The barbiturate decreases the effect of metabolized beta-blocker
Phenobarbital The barbiturate decreases the effect of metabolized beta-blocker
Primidone The barbiturate decreases the effect of metabolized beta-blocker
Quinidine barbiturate The barbiturate decreases the effect of metabolized beta-blocker
Secobarbital The barbiturate decreases the effect of metabolized beta-blocker
Talbutal The barbiturate decreases the effect of metabolized beta-blocker
Thioridazine Increased risk of cardiotoxicity and arrhythmias
Mesoridazine Increased risk of cardiotoxicity and arrhythmias
Citalopram The SSRI increases the effect of the beta-blocker
Escitalopram The SSRI increases the effect of the beta-blocker
Fluoxetine The SSRI increases the effect of the beta-blocker
Paroxetine The SSRI increases the effect of the beta-blocker
Sertraline The SSRI increases the effect of the beta-blocker
Dihydroergotamine Ischemia with risk of gangrene
Dihydroergotoxine Ischemia with risk of gangrene
Ergonovine Ischemia with risk of gangrene
Ergotamine Ischemia with risk of gangrene
Methysergide Ischemia with risk of gangrene
Ibuprofen Risk of inhibition of renal prostaglandins
Indomethacin Risk of inhibition of renal prostaglandins
Piroxicam Risk of inhibition of renal prostaglandins
Food Interactions: Avoid alcohol.
Take with food.
Avoid natural licorice.
Generic Name: Propranolol
Synonyms: Not Available
Drug Category: Vasodilator Agents; Anti-anxiety Agents; Antihypertensive Agents; Antiarrhythmic Agents; Adrenergic Agents
Drug Type: Small Molecule; Approved
Other Brand Names containing Propranolol: Angilol; Apsolol; Avlocardyl; Bedranol; Beprane; Berkolol; Beta-Neg; Beta-Propranolol; Beta-Tablinen; Beta-Timelets; Betachron; Betalong; Cardinol; Caridolol; Corpendol; Deralin; Dl-Propranolol Hydrochloride; Dociton; Duranol; Efektolol; Elbrol; Etalong; Euprovasin; Frekven; Inderal; Inderal La; Inderide; Indobloc; Innopran XL; Intermigran; Kemi S; Obsidan; Oposim; Prano-Puren; Propanalol; Propanix; Propanolol; Prophylux; Propranalol; Propranolol Hcl; Propranolol Hcl Intensol; Propranolol Hydrochloride; Propranur; Proprasylyt; Pylapron; R,S-Propranolol Hydrochloride; Rapynogen; Reducor; Reducor Line; Sagittol; Servanolol; Sloprolol; Sumial; Tesnol;
Absorption: Propranolol is almost completely absorbed from the GI tract; however, plasma concentrations attained are quite variable among individuals.
Toxicity (Overdose): Symptoms of overdose include bradycardia, cardiac failure, hypotension, and brochospasm. LD50=565 mg/kg (orally in mice).
Protein Binding: More than 90%
Half Life: 4 hours
Dosage Forms of Apsolol: Solution Intravenous
Capsule, extended release Oral
Chemical IUPAC Name: 1-naphthalen-1-yloxy-3-(propan-2-ylamino)propan-2-ol
Chemical Formula: C16H21NO2
Propranolol on Wikipedia: http://en.wikipedia.org/wiki/Propranolol
Organisms Affected: Humans and other mammals