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Propranolol (INN
International Nonproprietary Name

An International Nonproprietary Name is the official non-proprietary or generic name given to a pharmaceutical substance, as designated by the World Health Organization ....
) is a non-selective beta blocker
Beta blocker

Beta blockers are a class of medication used for various indications, but particularly for the management of cardiac arrhythmias, cardioprotection after myocardial infarction , and hypertension....
 mainly used in the treatment of hypertension
Hypertension

Hypertension, also referred to as high blood pressure, HTN or HPN, is a medical condition in which the blood pressure is chronically elevated....
. It was the first successful beta blocker developed. It is the only drug proven effective for the prophylaxis
Prophylaxis

Prophylaxis is any medical or public health procedure whose purpose is to prevent, rather than treat or cure a disease. Roughly, prophylactic measures are divided between primary prophylaxis and secondary prophylaxis ....
 of migraines in children. Propranolol is available in generic form as propranolol hydrochloride, as well as an AstraZeneca
AstraZeneca

AstraZeneca plc , is a large Anglo-Swedish pharmaceutical company formed on 6 April 1999 by the remerger of Swedish Astra AB and British Zeneca Group plc....
 and Wyeth
Wyeth

Wyeth, formerly known as American Home Products , is one of the largest pharmaceutical company in the world. The company is based in Madison, New Jersey....
 product under the trade name
Trade name

A trade name, also known as a trading name or a business name, is the name which a business trades under for commercial purposes, although its registered, Legal name , used for contracts and other formal situations, may be another....
s Inderal, Inderal LA, Avlocardyl (also available in prolonged absorption form named "Avlocardyl Retard"), Deralin, Dociton, Inderalici, InnoPran XL, Sumial (depending on marketplace and release rate).

lass="link1" onMouseover='showByLink("m855251",this)' onMouseout='hide("m855251")'href="http://www.absoluteastronomy.com/topics/Scotland">Scottish
Scotland

conventional_long_name = ScotlandAlba|common_name= Scotland|image_flag = Flag of Scotland.svg|flag_width = 130px...
 scientist and St.






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Propranolol (INN
International Nonproprietary Name

An International Nonproprietary Name is the official non-proprietary or generic name given to a pharmaceutical substance, as designated by the World Health Organization ....
) is a non-selective beta blocker
Beta blocker

Beta blockers are a class of medication used for various indications, but particularly for the management of cardiac arrhythmias, cardioprotection after myocardial infarction , and hypertension....
 mainly used in the treatment of hypertension
Hypertension

Hypertension, also referred to as high blood pressure, HTN or HPN, is a medical condition in which the blood pressure is chronically elevated....
. It was the first successful beta blocker developed. It is the only drug proven effective for the prophylaxis
Prophylaxis

Prophylaxis is any medical or public health procedure whose purpose is to prevent, rather than treat or cure a disease. Roughly, prophylactic measures are divided between primary prophylaxis and secondary prophylaxis ....
 of migraines in children. Propranolol is available in generic form as propranolol hydrochloride, as well as an AstraZeneca
AstraZeneca

AstraZeneca plc , is a large Anglo-Swedish pharmaceutical company formed on 6 April 1999 by the remerger of Swedish Astra AB and British Zeneca Group plc....
 and Wyeth
Wyeth

Wyeth, formerly known as American Home Products , is one of the largest pharmaceutical company in the world. The company is based in Madison, New Jersey....
 product under the trade name
Trade name

A trade name, also known as a trading name or a business name, is the name which a business trades under for commercial purposes, although its registered, Legal name , used for contracts and other formal situations, may be another....
s Inderal, Inderal LA, Avlocardyl (also available in prolonged absorption form named "Avlocardyl Retard"), Deralin, Dociton, Inderalici, InnoPran XL, Sumial (depending on marketplace and release rate).

History and development

Scottish
Scotland

conventional_long_name = ScotlandAlba|common_name= Scotland|image_flag = Flag of Scotland.svg|flag_width = 130px...
 scientist and St. Andrews graduate James W. Black
James W. Black

Sir James Whyte Black, Order of Merit, Royal Society, Royal Society of Edinburgh, Royal College of Physicians is a Scotland Physician and Pharmacology who invented Propranolol, synthesized Cimetidine and was awarded the Nobel Prize in Physiology or Medicine in 1988 for these discoveries....
 successfully developed propranolol in the late 1950s. He was awarded the Nobel Prize in Medicine for this discovery in 1988. Propranolol was derived from the early ß-adrenergic antagonists dichloroisoprenaline
Dichloroisoprenaline

Dichloroisoprenaline, also known as dichlorosisoproterenol or DCI, was the first compound developed that exhibited ?-adrenergic receptor antagonist activity....
 and pronethalol
Pronethalol

Pronethalol was an early beta blocker clinical candidate. It was never used clinically due to carcinogenicity in mice.References...
. The key structural modification, which was carried through to essentially all subsequent beta blockers, was the insertion of an oxymethylene bridge into the arylethanolamine structure of pronethalol thus greatly increasing the potency of the compound. This also apparently eliminated the carcinogenicity found with pronethalol in animal models.

Newer, more selective beta-blockers (such as nebivolol
Nebivolol

Nebivolol is a highly cardioselective beta blocker with nitric oxide-potentiating vasodilatory effect used in treatment of hypertension and, in Europe, also for left ventricular failure....
) are now used in the treatment of hypertension.

Pharmacology


Propranolol is a non-selective beta blocker
Beta blocker

Beta blockers are a class of medication used for various indications, but particularly for the management of cardiac arrhythmias, cardioprotection after myocardial infarction , and hypertension....
, that is, it blocks the action of epinephrine
Epinephrine

Epinephrine is a hormone and neurotransmitter.Epinephrine increases the "fight or flight" response of the Sympathetic nervous system of the autonomic nervous system....
 on both ß1- and ß2-adrenergic receptor
Adrenergic receptor

The adrenergic receptors are a class of G protein-coupled receptors that are targets of the catecholamines. Adrenergic Receptor s specifically bind and are activated by their endogenous ligands, the catecholamines adrenaline and noradrenaline ....
s. It has little intrinsic sympathomimetic activity (ISA) but has strong membrane stabilizing activity (only at high blood concentrations, eg overdosage). Only L-propranolol is a powerful adrenoceptor antagonist, whereas D-propranolol is not. However, both have local anesthetic
Local anesthetic

A local anesthetic is a medication that causes reversible local anesthesia and a loss of nociception. When it is used on specific nerve pathways , effects such as analgesia and paralysis can be achieved....
 (termed topical) effect.

Pharmacokinetics

Propranolol is rapidly and completely absorbed, with peak plasma levels achieved approximately 1–3 hours after ingestion. Co-administration with food appears to enhance bioavailability. Despite complete absorption, propranolol has a variable bioavailability
Bioavailability

In pharmacology, bioavailability is used to describe the fraction of an administered dose of unchanged drug that reaches the systemic circulation, one of the principal pharmacokinetics properties of medication....
 due to extensive first-pass metabolism. Hepatic impairment will therefore increase its bioavailability. The main metabolite 4-hydroxypropranolol, with a longer half-life
Half-life

The half-life of a quantity whose value decreases with time is the interval required for the quantity to decay to half of its initial value. The concept originated in describing how long it takes atoms to undergo radioactive decay but also applies in a wide variety of other situations....
 (5.2–7.5 hours) than the parent compound (3–4 hours), is also pharmacologically active.

Propranolol is a highly lipophilic
Lipophilic

Lipophilicity, , refers to the ability of a chemical compound to dissolve in fats, oils, lipids, and non-polar solvents such as hexane or toluene....
 drug achieving high concentrations in the brain. The duration of action of a single oral dose is longer than the half-life and may be up to 12 hours, if the single dose is high enough (e.g., 80 mg). Effective plasma concentrations are between 10–100 ng/mL.

Toxic levels are associated with plasma concentrations above 2000 ng/ml.

Clinical use


Indications

Propranolol is indicated for the management of various conditions including:
  • Hypertension
    Hypertension

    Hypertension, also referred to as high blood pressure, HTN or HPN, is a medical condition in which the blood pressure is chronically elevated....
  • Angina pectoris
  • Tachyarrhythmias
  • Myocardial infarction
    Myocardial infarction

    Myocardial infarction , commonly known as a heart attack, occurs when the Blood flow to part of the heart is interrupted. This is most commonly due to occlusion of a coronary artery following the rupture of a Vulnerable plaque, which is an unstable collection of lipids and white blood cells in the wall of an artery....
  • Control of tachycardia
    Tachycardia

    The word tachycardia comes from the Greek words tachys and kardia .Tachycardia typically refers to a heartrate that exceeds the range of the normal resting heartrate, based upon age:...
    /tremor associated with anxiety
    Anxiety

    Anxiety is a psychological and physiological state characterized by cognitive, somatic, emotional, and behavioral components. These components combine to create an unpleasant feeling that is typically associated with uneasiness, fear, or worry....
    , hyperthyroidism
    Hyperthyroidism

    Hyperthyroidism is the term for overactive tissue within the thyroid gland,resulting in overproduction and thus an excess of circulating free thyroid hormones: thyroxine , triiodothyronine , or both....
     or lithium therapy
    Lithium pharmacology

    Lithium pharmacology refers to use of the lithium ion, Li+, as a drug. A number of chemical salts of lithium are used medically as a mood stabilizer Medication, primarily in the treatment of bipolar disorder, where they have a role in the treatment of Clinical depression and particularly of mania, both acutely and in the long term....
    .
  • Essential tremor
    Essential tremor

    Essential tremor is a progressive neurological disorder whose most recognizable feature is a tremor of the arms that is apparent during voluntary movements such as eating and writing....
  • Migraine
    Migraine

    Migraine is a neurology syndrome characterized by altered bodily perceptions, headaches, and nausea. Physiologically, the migraine headache is a neurological condition more common to women than to men....
     prophylaxis
  • Cluster Headaches prophylaxis
  • Tension headache
    Tension headache

    Tension headaches, which were renamed tension-type headaches by the International Headache Society in 1988, are the most common type of primary headaches....
     (Off the label use)
  • Tetralogy of Fallot
    Tetralogy of Fallot

    Tetralogy of Fallot is a congenital heart defect which is classically understood to involve four anatomical abnormalities . It is the most common Cyanosis heart defect, representing 55-70%, and the most common cause of blue baby syndrome....
  • Phaeochromocytoma (along with a blocker
    Alpha blocker

    Alpha-1 blockers constitute a variety of drugs which block Adrenergic receptor#Alpha .CE.B1 receptors in arteries and smooth muscles....
    )
  • There has been some experimentation in psychiatric areas:
    • Treating the excessive drinking of fluids in psychogenic polydipsia
      Psychogenic polydipsia

      Psychogenic polydipsia is a special form of polydipsia, caused by mental disorders....
      ,
    • Antipsychotic
      Antipsychotic

      Antipsychotics are a group of psychoactive drugs commonly but not exclusively used to treat psychosis, which is typified by schizophrenia. Over time a wide range of antipsychotics have been developed....
      -induced akathisia
      Akathisia

      Akathisia, or acathisia, is a syndrome characterized by unpleasant sensations of "inner" restlessness that manifests itself with an inability to sit still or remain motionless, hence its origin in Ancient Greek a , [without, not] + ????s?? , [sitting]....
      ,
    • Aggressive behavior of patients with brain injuries
    • Post-traumatic stress disorder
      Post-traumatic stress disorder

      Posttraumatic stress disorder is an anxiety disorder that can develop after exposure to one or more traumatic events that threatened or caused grave physical harm....
  • Glaucoma
    Glaucoma

    Glaucoma is a group of diseases of the optic nerve involving loss of ganglion cell in a characteristic pattern of optic atrophy. Raised intraocular pressure is a significant risk factor for developing glaucoma ....


While once first-line treatment for hypertension
Hypertension

Hypertension, also referred to as high blood pressure, HTN or HPN, is a medical condition in which the blood pressure is chronically elevated....
, the role for beta-blockers was downgraded in June 2006 in the United Kingdom
United Kingdom

The United Kingdom of Great Britain and Northern Ireland, commonly known as the United Kingdom , the UK or Britain,is a sovereign state located off the northwestern coast of continental Europe....
 to fourth-line as they perform less well than other drugs, particularly in the elderly, and evidence is increasing that the most frequently used beta-blockers at usual doses carry an unacceptable risk of provoking type 2 diabetes
Diabetes mellitus type 2

Diabetes mellitus type 2 or type 2 diabetes is a metabolism metabolic disorder that is characterized by high blood glucose in the context of insulin resistance and relative insulin deficiency....
.

Propranolol is also used to lower portal vein
Hepatic portal vein

The hepatic portal vein is a vein in the abdominal cavity that drains blood from the gastrointestinal tract and spleen. It is usually formed by the confluence of the superior mesenteric vein and splenic veins, and also receives blood from the inferior mesenteric vein, gastric vein, and cystic veins....
 pressure in portal hypertension
Portal hypertension

In medicine, portal hypertension is hypertension in the portal vein and its tributaries.It is often defined as a portal pressure gradient of 5 mm Hg or greater....
 and prevent oesophageal variceal
Esophageal varices

In medicine , esophageal varices are extremely dilation sub-mucosal veins in the esophagus. They are most often a consequence of portal hypertension, such as may be seen with cirrhosis; patients with esophageal varices have a strong tendency to develop bleeding....
 bleeding.

Propranolol is often used by musicians and other performers to prevent stage fright
Stage fright

Stage fright or performance anxiety is the anxiety, fear, or persistent phobia which may be aroused in an individual by the requirement to performance in front of an audience, whether actually or potentially ....
.

Propranolol is currently being investigated as a potential treatment for post-traumatic stress disorder
Post-traumatic stress disorder

Posttraumatic stress disorder is an anxiety disorder that can develop after exposure to one or more traumatic events that threatened or caused grave physical harm....
.

Precautions/contraindications


Propranolol should be used with caution in patients with:

  • Diabetes mellitus
    Diabetes mellitus

    Diabetes mellitus , often referred to simply as diabetes , is a syndrome of disordered metabolism, usually due to a combination of genetic disorder and environmental causes, resulting in abnormally high blood sugar levels ....
     or hyperthyroidism
    Hyperthyroidism

    Hyperthyroidism is the term for overactive tissue within the thyroid gland,resulting in overproduction and thus an excess of circulating free thyroid hormones: thyroxine , triiodothyronine , or both....
    , since signs and symptoms of hypoglycaemia may be masked. Also, propranolol may affect blood sugar levels
  • Peripheral vascular disease and Raynaud's syndrome, which may be exacerbated
  • Phaeochromocytoma, as hypertension
    Hypertension

    Hypertension, also referred to as high blood pressure, HTN or HPN, is a medical condition in which the blood pressure is chronically elevated....
     may be aggravated without prior alpha blocker
    Alpha blocker

    Alpha-1 blockers constitute a variety of drugs which block Adrenergic receptor#Alpha .CE.B1 receptors in arteries and smooth muscles....
     therapy
  • Myasthenia gravis
    Myasthenia gravis

    Myasthenia gravis is a neuromuscular disease leading to fluctuating muscle weakness and fatigue . It is an autoimmunity, in which weakness is caused by circulating antibody that block acetylcholine receptors at the post-synaptic neuromuscular junction, inhibiting the stimulative effect of the neurotransmitter acetylcholine....
    , may be worsened
  • Other drugs with bradycardic
    Bradycardia

    Bradycardia , as applied to adult medicine, is defined as a resting heart rate of under 60 beats per minute, though it is seldom symptomatic until the rate drops below 50 beat/min....
     effects


Propranolol is contraindicated in patients with:

  • Reversible airways disease, particularly asthma
    Asthma

    Asthma is a common chronic obstructive pulmonary disease, in which the Lung constrict, become inflammation, and are lined with excessive amounts of thickened mucus, often in response to one or more triggers....
     or chronic obstructive pulmonary disease (COPD)
  • Bradycardia
    Bradycardia

    Bradycardia , as applied to adult medicine, is defined as a resting heart rate of under 60 beats per minute, though it is seldom symptomatic until the rate drops below 50 beat/min....
     (<50 beats/minute)
  • Sick sinus syndrome
    Sick sinus syndrome

    Sick sinus syndrome, also called sinus node dysfunction, is a group of abnormal heart rhythms presumably caused by a malfunction of the sinus node, the heart's primary pacemaker....
  • Atrioventricular block
    Atrioventricular block

    An atrioventricular block is a type of heart block involving impairment of the conduction between the atria and ventricles of the heart. It usually involves the atrioventricular node, but it can involve other structures....
     (second or third degree)
  • Shock
  • Severe hypotension
    Hypotension

    In physiology and medicine, hypotension refers to an abnormally low blood pressure. This is best understood as a physiologic state, rather than a disease....
  • Uncontrolled congestive heart failure
    Congestive heart failure

    Heart failure is a condition in which a problem with the structure or function of the heart impairs its ability to supply sufficient blood flow to meet the body's needs....
  • Cocaine toxicity [per American Heart Association guidelines, 2005]


Adverse effects

Adverse drug reaction
Adverse drug reaction

An adverse drug reaction or adverse drug event is an expression that describes the unwanted, negative consequences associated with the use of given medications....
s (ADRs) associated with propranolol therapy are similar to other lipophilic beta blockers (see beta blocker
Beta blocker

Beta blockers are a class of medication used for various indications, but particularly for the management of cardiac arrhythmias, cardioprotection after myocardial infarction , and hypertension....
).

Pregnancy and lactation

Propranolol, like other beta blockers, is classified as Pregnancy category
Pregnancy category

The pregnancy category of a medication agent is an assessment of the risk of fetal injury due to the pharmaceutical, if it is used as directed by the mother during pregnancy....
 C in the United States and ADEC
Australian Drug Evaluation Committee

The Australian Drug Evaluation Committee or ADEC, is a committee that provides independent scientific advice to the Government of Australia regarding therapeutic medication....
 Category C in Australia. Beta-blocking agents in general reduce perfusion of the placenta which may lead to adverse outcomes for the neonate, including pulmonary or cardiac complications, or premature birth. The newborn may experience additional adverse effects such as hypoglycemia
Hypoglycemia

Hypoglycaemia or hypoglycemia is the medical term for a Pathology state produced by a lower than normal level of Blood glucose. The term hypoglycemia literally means "under-sweet blood" ....
 and bradycardia
Bradycardia

Bradycardia , as applied to adult medicine, is defined as a resting heart rate of under 60 beats per minute, though it is seldom symptomatic until the rate drops below 50 beat/min....
.

Most beta-blocking agents appear in the milk of lactating
Lactation

Lactation describes the secretion of milk from the mammary glands, the process of providing that milk to the young, and the period of time that a mother lactates to feed her young....
 women. This is especially the case for a lipophilic
Lipophilic

Lipophilicity, , refers to the ability of a chemical compound to dissolve in fats, oils, lipids, and non-polar solvents such as hexane or toluene....
 drug like propranolol. Breastfeeding is not recommended in patients receiving propranolol therapy.

Interactions

Beta blockers, including propranolol, have an additive effect with other drugs which decrease blood pressure, or which decrease cardiac contractility or conductivity. Clinically-significant interactions particularly occur with:

  • verapamil
    Verapamil

    Verapamil is an L-type calcium channel blocker of the phenylalkylamine class. It has been used in the treatment of hypertension, angina pectoris, cardiac arrhythmia, and most recently, cluster headaches....
  • epinephrine
    Epinephrine

    Epinephrine is a hormone and neurotransmitter.Epinephrine increases the "fight or flight" response of the Sympathetic nervous system of the autonomic nervous system....
  • ß2-adrenergic receptor agonists
    Beta2-adrenergic receptor agonist

    Beta2-adrenergic agonists, also known as Beta2-adrenergic receptor agonists, are a class of medication used to treat asthma and other lung disease states....
  • clonidine
    Clonidine

    Clonidine is a direct-acting alpha-2 adrenergic receptor adrenergic agonist....
  • ergot alkaloids
  • isoprenaline
  • non-steroidal anti-inflammatory drug
    Non-steroidal anti-inflammatory drug

    Non-steroidal anti-inflammatory drugs, usually abbreviated to NSAIDs or NAIDs, are Medications with analgesic, antipyretic and, in higher doses, with anti-inflammatory effects ....
    s
  • quinidine
    Quinidine

    Quinidine is a pharmaceutical Medication that acts as a class I antiarrhythmic agent in the heart. It is a stereoisomer of quinine, originally derived from the bark of the cinchona tree....
  • cimetidine
    Cimetidine

    Cimetidine is a histamine H2-receptor antagonist that inhibits the production of acid in the stomach. It is largely used in the treatment of heartburn and peptic ulcers....
  • lidocaine
    Lidocaine

    Lidocaine or lignocaine is a common local anesthetic and antiarrhythmic agent drug. Lidocaine is used topically to relieve itching, burning and pain from skin inflammations, injected as a dental anesthetic, and in minor surgery....
  • phenobarbital
    Phenobarbital

    Phenobarbital or phenobarbitone is a barbiturate, first marketed as Luminal by Bayer. It is the most widely used anticonvulsant worldwide and the oldest still commonly used....
  • rifampicin
    Rifampicin

    Rifampicin or rifampin is a bactericidal antibiotic drug of the rifamycin group. It is a semisynthetic compound derived from Amycolatopsis rifamycinica ....
  • Fluvoxamine
    Fluvoxamine

    Fluvoxamine is an antidepressant which functions as a selective serotonin reuptake inhibitor. It is most often used to treat obsessive-compulsive disorder....
     slows down the metabolism of propranolol significantly leading to increased blood levels of propranolol.


Dosage

The usual maintenance dose ranges for oral propranolol therapy vary by indication:

  • Hypertension, angina, essential tremor
    • 120–320 mg daily in divided doses
    • Sustained-release formulations are available in some markets.


  • Tachyarrhythmia, anxiety (GAD), hyperthyroidism
    • 10–40 mg 3–4 times daily


  • Performance anxiety
    • 5-10 mg 30min or 1.5hrs before and after performance, optionally 5-10 mg night before.


Intravenous (IV) propranolol may be used in acute arrhythmia or thyrotoxic crisis
Hyperthyroidism

Hyperthyroidism is the term for overactive tissue within the thyroid gland,resulting in overproduction and thus an excess of circulating free thyroid hormones: thyroxine , triiodothyronine , or both....
.

Research into role against malaria

Propranolol along with a number of other membrane-acting drugs have been investigated for possible effects on P. falciparum
Plasmodium falciparum

Plasmodium falciparum is a protozoan parasite, one of the species of Plasmodium that cause malaria in humans. It is transmitted by the female...
 and so the treatment of malaria
Malaria

Malaria is a Vector -borne infectious disease caused by protozoan parasites. It is widespread in Tropics and subtropical regions, including parts of the Americas, Asia, and Africa....
. In vitro positive effects until recently had not been matched by useful in vivo anti-parasite activity against P. vinckei
Plasmodium vinckei

Plasmodium accipiteris is a parasite of the genus Plasmodium subgenus Vinckeia.Like all Plasmodium species P. vinckei has both vertebrate and insect hosts....
, or P. yoelii nigeriensis
Plasmodium yoelii

Plasmodium achiotense is a parasite of the genus Plasmodium subgenus Vinckeia.Like all Plasmodium species P. yoelii has both vertebrate and insect hosts....
. However a single study from 2006 has suggested that propranolol may reduce the dosages required for existing drugs to be effective against P. falciparum by 5- to 10-fold, suggesting a role for combination therapies.

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