Propranolol , sold under the brand name Inderal among others, is a beta-blocker type of drug. It is used to treat high blood pressure, a number of types of irregular heartbeat, thyrotoxicosis, capillary hemangioma, performance anxiety, and essential tremor. It is used to prevent migraine headaches, and to prevent further heart problems in those with angina or previous heart attacks. Can be taken by mouth or by injection into a blood vessel. The formulations taken by the mouth come in short acting versions and long-acting. Propranolol appears in the blood after 30 minutes and has a maximum effect of 60 and 90 minutes when taken.
Common side effects include nausea, abdominal pain, and constipation. It should not be used on those with slow heart rates and most of them with heart failure. Stopping drugs quickly in those with coronary artery disease may worsen the symptoms. This can worsen the symptoms of asthma. Caution is recommended in those with liver or kidney problems. Propranolol may cause harmful effects on infants if taken during pregnancy. Use during breastfeeding may be safe, but infants should be monitored for side effects. This is a non-selective beta blocker that works by blocking adrenergic receptors.
Propranolol was discovered in 1964. It is a List of Essential Medicines of the World Health Organization, the most effective and safe medicines needed in the health system. Propranolol is available as a generic drug. Wholesale costs in developing countries are between US $ 0.24 and US $ 2.16 per month in 2014. In the United States it costs around $ 15 per month at typical doses.
Video Propranolol
Medical use
Propranolol is used to treat a variety of conditions, including:
Cardiovascular
- Hypertension
- Angina pectoris (with the exception of variant angina)
- Tachyarrhythmia
- Myocardial infarction
- Tachycardia (and symptoms of other sympathetic nervous systems, such as muscle tremors) are associated with a variety of conditions, including anxiety, panic, hyperthyroidism, and lithium therapy
- Portal hypertension, to lower portal venous pressure
- Prevention of bleeding of esophageal and ascites esophageal
- Anxiety
- Hypertrophic cardiomyopathy
While once first-line treatment for hypertension, the role for beta blockers was lowered in June 2006 in the UK to the fourth row, as they did not perform as well as other drugs, especially in the elderly, and evidence increased that the beta blockers most frequently used at regular doses carry an unacceptable risk to provoke type 2 diabetes.
Propranolol is not recommended for the treatment of hypertension by the Eighth Joint National Committee (JNC 8) because of higher rates of major composite results of cardiovascular death, myocardial infarction, or stroke compared with angiotensin receptor blockers recorded in one study.
Psychiatry
Propranolol is sometimes used to treat performance anxiety. The evidence to support its use in other anxiety disorders is poor. Several experiments have been conducted in other psychiatric fields:
- Post-traumatic stress disorder (PTSD) and specific phobias (see subsections below)
- Aggressive behavior of patients with brain injury
- Treating excessive fluid drinking at psychogenic polidipsia
PTSD and phobia
Propranolol is being investigated as a potential treatment for PTSD. Propranolol works to inhibit the action of norepinephrine, a neurotransmitter that improves memory consolidation. In one small study, individuals were administered propranolol immediately after the trauma experienced fewer stress-related symptoms and lower PTSD levels than the control group who did not receive the drug. Due to the fact that their emotional memories and content are consolidated within hours of being remembered/re-experienced, propranolol can also reduce the emotional impact of the memories already established; for this reason, it is also being studied in the treatment of specific phobias, such as arachnophobia, dental fear, and social phobia.
Ethical and legal questions have been raised around the use of drug-based propranolol for use as "memory absorbers", including: altering memory memories during inquiry, modifying behavioral responses to past experiences (although traumatic), arranging these drugs, and others. However, Hall and Carter argue that many such objections "are based on overly unrealistic scenarios that ignore the limited action of propranolol in influencing memory, downplay the debilitating effects that PTSD has on those who suffer, and fail to acknowledge the extent to which drugs such as alcohol already used for this purpose. "
More
- Tremors are important. Evidence to use for akathisia is not enough
- Migraine and prevention of cluster headaches and extra work headaches
- Hyperhidrosis (excessive sweating)
- Breeds infantile hemangiomas
- Glaucoma
- Thyrotoxicosis by inhibition of deiodinase
Propranolol may be used to treat severe infantile hemangioma (IHs). This treatment shows promise as superior to corticosteroids when treating IHs. Evidence of extensive clinical cases and small controlled trials support their efficacy.
Maps Propranolol
Contraindications
Propranolol can be contraindicated in people with:
- Reversible airway disease, particularly asthma or chronic obstructive pulmonary disease (COPD)
- Slow heart rate (bradycardia) (& lt; 60 beats/min)
- Pain sick syndrome
- Atrioventricular block (second or third degree)
- Shock
- Severe low blood pressure
- Cocaine toxicity [per American Heart Association guidelines, 2005]
Adverse effects
Propranolol should be used with caution in people with:
- Diabetes mellitus or hyperthyroidism, as signs and symptoms of hypoglycemia may be disguised
- Peripheral vascular disease and Raynaud's syndrome, which may get worse
- Phaeochromocytoma, because hypertension can be aggravated without previous alpha blocker therapy
- Myasthenia gravis, which may get worse
- Other drugs with bradycardic effects
Pregnancy and lactation
Propranolol, like other beta blockers, is classified as the category of pregnancy C in the United States and the category of ADEC C in Australia. ? block-breaking agents generally reduce placental perfusion, which can lead to adverse outcomes for neonates, including lung or cardiac complications, or premature birth. Newborns may experience additional side effects such as low blood sugar and slower than a normal heartbeat.
Most of the -blocking agents appear in the milk of lactating women. However, propranolol is strongly bound to proteins in the bloodstream and is distributed to breast milk at very low levels. This low rate is not expected to pose a risk to breastfeeding infants, and the American Academy of Pediatrics considers propranolol therapy "generally compatible with breastfeeding".
Because of the high penetration in the blood-brain barrier, lipophilic beta inhibitors such as propranolol and metoprolol are more likely than other lipophilic lipid beta-causing sleep disorders such as insomnia and clear dreams, and nightmares. Dreaming (rapid eye movement sleep, REM) is reduced and awareness increases.
Adverse drug reactions associated with propranolol therapy are similar to other lipophilic beta blockers.
Overdose
In propranolol an overdose is associated with seizures. Cardiac arrest may occur in an overdose of propranolol due to sudden ventricular arrhythmias, or cardiogenic shock that can eventually peak in the bradicardic PEA. Propranolol should be used with extreme caution in patients with depression or patients with atypical depression with a possible suicidal idea.
Interactions
Because beta blockers are known to relax the heart muscle and constrict smooth muscle, beta-adrenergic antagonists, including propranolol, have additive effects with other drugs that lower blood pressure, or that decrease contractility or cardiac conductivity. Significant clinical interactions typically occur with:
- Verapamil
- Epinephrine (adrenaline)
- ? 2 adrenergic receptor agonist
- Salbutamol, levosalbutamol, formoterol, salmeterol, clenbuterol etc.
- Clonidine
- Ergot alkaloid
- Isoprenalin (isoproterenol)
- Non-steroidal anti-inflammatory drugs (NSAIDs)
- Quinidine
- Cimetidine
- Lidocaine
- Phenobarbital
- Rifampicin
- Fluvoxamine (significantly slows propranolol metabolism, leading to elevated blood levels of propranolol)
Pharmacology
Pharmacodynamics
Propranolol is classified as a non-cardioselective beta-sympatholytic blocker that crosses the blood-brain barrier. It is fat soluble and also has the effect of blocking sodium channels. Propranolol is a non-selective beta blocker; ie blocking the action of epinephrine (adrenaline) and norepinephrine (noradrenaline) in the adrenergic receptors well 1 - and? 2 . It has little intrinsic sympathomimetic activity, but has a strong membrane stabilization activity (only in high blood concentrations, eg overdose). Propranolol is able to cross the blood-brain barrier and exert an effect in the central nervous system in addition to its peripheral activity.
In addition to the adrenergic receptor blockade, propranolol has a very weak inhibitory effect on norepinephrine and/or weak transporters stimulating norepinephrine release (ie, norepinephrine concentration increases in the synapse). Because of propranolol block? -adrenoceptor, the increase in synaptic norepinephrine only results in "activation -adrenoceptors", with " 1 -adrenoceptors become very important for the observed effects on the animal model.Hence, it can be seen as weak indirectly < > 1 -adrenoceptor agonist other than strong? -adrenoceptor antagonist.In addition to its effect on adrenergic system, there is evidence to suggest that propranolol may act as a weak antagonist of certain serotonin receptors, ie 5-HT 1A , 5-HT 1B , and prescription 5-HT 2B .The latter may be involved in the effectiveness of propranolol in the treatment of migraine at high doses.
Both propranolol enantiomers have local (topical) anesthetic effects, which are usually mediated by a blocked-voltage gated sodium blockade. Research has demonstrated the ability of propranolol to block the sodium channels of the heart, nerve, and skeletal nerves, explaining the known effect of membrane stabilization and the effects of the central nervous system and other antiarrhythmias.
Pharmacokinetics
Propranolol is absorbed rapidly and perfectly, with peak plasma levels being achieved about 1-3 hours after consumption. Giving along with food seems to increase bioavailability. Despite complete absorption, propranolol has variable bioavailability because of extensive first-pass metabolism. Liver damage therefore increases its bioavailability. The main 4-hydroxypropranolol metabolite, with a longer half-life (5.2-7.5 hours) than the parent compound (3-4 hours), is also pharmacologically active.
Propranolol is a highly lipophilic drug that achieves high concentrations in the brain. The duration of a single oral dose action is longer than part-time and may be up to 12 hours, if a single dose is high enough (eg, 80 mg). Effective plasma concentrations are between 10 and 100 mg/l. Toxic levels are associated with plasma concentrations above 2000 mg/l.
History
British scientist James W. Black developed propranolol in the 1960s. In 1988, he was awarded the Nobel Prize in Medicine for this discovery. Propranolol is inspired by the early anthrags of dichloroisoprenaline and pronethalol. The main difference, carried through basically all subsequent beta blockers, is the inclusion of oxymethylene (-O-CH 2 -) groups between aryl groups and ethanolamine from pronethalol, greatly increasing the potential of the compound. It also seems to eliminate the carcinogenicity found with pronethalol in animal models.
More recently, more cardiac selective beta blockers (such as bisoprolol, nebivolol, carvedilol, or metoprolol) are now used in the treatment of hypertension.
Society and culture
In a 1987 study by the Symphony International Conference and Opera Musicians, it was shown that 27% of interviewed members admitted using a beta blocker such as propranolol for musical performances. For about 10-16% of players, their stage fright levels are considered pathological. Propranolol is used by musicians, actors, and public speakers because of its ability to treat anxiety symptoms that are activated by the sympathetic nervous system.
Brand name
Original propranolol was marketed in 1965 under the Inderal brand and produced by ICI Pharmaceuticals (now AstraZeneca). Propranolol is also marketed under the trademarks Avlocardyl, Deralin, Dociton, Inderalici, InnoPran XL, Sumial, Anaprilin, and Bedranol SR (Sandoz). In India marketed under brand names like Ciplar and Ciplar LA by Cipla. Hemangeol, a propranolol solution of 4.28 mg/mL, is indicated for the treatment of infantile hemangiomas that proliferate.
Research
Clinical research has been done to find out whether propranolol can be useful in the treatment of some cancers.
References
External links
- Stapleton MP (1997). "Sir James Black and propranolol The role of basic sciences in the history of cardiovascular pharmacology". Texas Heart Institute Journal . 24 (4): 336-42. PMC 325477 . PMID 9456487. Ã,
- US. National Library of Medicine: Drug Information Portal - Propranolol
Source of the article : Wikipedia
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