What class of drug is mecamylamine?
Mecamylamine belongs to a class of drugs known as ganglion blockers. It works by relaxing blood vessels so blood can flow more easily.
Is mecamylamine a competitive antagonist?
Mecamylamine (MEC) is a ganglionic blocker that has been used as an anti-hypertensive agent (Inversine®) and is known to be a non-competitive antagonist of several nicotinic acetylcholine receptors (nAChR) including the α4β2 receptor (Sacco et al., 2004).
Does mecamylamine contain nicotine?
Mecamylamine is a nicotine antagonist (that is, it blocks the effect of nicotine). The rationale for its use in smoking cessation is that it may block the rewarding effect of nicotine and thus reduce the urge to smoke.
What does mecamylamine target?
Mecamylamine crosses the blood-brain and placental barriers. Mecamylamine is a ganglionic blocker which prevents stimulation of postsynaptic receptors by acetylcholine released from presynaptic nerve endings….Pharmacology.
|ANeuronal acetylcholine receptor subunit alpha-2||antagonist||Humans|
What are contraindications of mecamylamine?
INVERSINE (mecamylamine) should not be used in mild, moderate, labile hypertension and may prove unsuitable in uncooperative patients. It is contraindicated in coronary insufficiency or recent myocardial infarction.
Is nicotine a ganglionic blocker?
Some substances can exhibit both stimulating and blocking effects on autonomic ganglia, depending on dosage and/or duration of action. An example for such a “dual” action is nicotine, which does this via depolarization block (see classification below).
What is the brand name for glycopyrrolate?
Glycopyrrolate is available under the following different brand names: Cuvposa, glycopyrronium, and Robinul.
What is Propantheline bromide used for?
Pro-Banthine tablets contain the active ingredient propantheline bromide which belongs to a group of drugs known as “antispasmodics”. They work by relaxing the muscles of the intestines. Pro-Banthine tablets are used to treat disorders in the gastrointestinal tract which involve muscle spasm.
Can malignant hypertension be reversed?
Malignant hypertension is a serious condition caused by very high blood pressure. It can quickly cause serious damage to eyes, kidneys and brain. Some of the changes can be reversed by treatment but some permanent damage may occur.
How do you manage malignant hypertension?
Patients with malignant hypertension are usually admitted to an intensive care unit for continuous cardiac monitoring, frequent assessment of neurologic status and urine output, and administration of intravenous antihypertensive medications and fluids.
When was mecamylamine introduced as an antihypertensive drug?
Mecamylamine ( INN, BAN; or mecamylamine hydrochloride ( USAN ); brand names Inversine, Vecamyl) is a non-selective, non-competitive antagonist of the nicotinic acetylcholine receptors (nAChRs) that was introduced in the 1950s as an antihypertensive drug.
How is mecamylamine related to the mesolimbic pathway?
Cholinergic signaling through nAChR in the mesolimbic pathway is involved with drug abuse reward effects like nicotine and cocaine. Studies in rats with mecamylamine, a nAChR nonselective antagonist, inhibit CPP and behavioral sensitization induced by cocaine.
What is the PK Ah of mecamylamine?
Chemically, mecamylamine is a secondary aliphatic amine, with a pK aH of 11.2 Mecamylamine has been used as an orally-active ganglionic blocker in treating autonomic dysreflexia and hypertension, but, like most ganglionic blockers, it is more often used now as a research tool.
How is mecamylamine used as a nAChR antagonist?
Mecamylamine, a noncompetitive and nonspecific nAChR antagonist, was seminal in establishing the involvement of nAChRs in relation to effects of alcohol in the mesocorticolimbic pathway.