Muscarinic antagonists

Ketamine is a cyclohexanone-derived general anesthetic and NMDA receptor antagonist with analgesic and hallucinogenic properties, used medically for anesthesia, depression, and pain management. Ketamine exists as its two enantiomers, S- (esketamine) and R- (arketamine), and has antidepressant action likely involving other mechanisms in addition to NMDA antagonism.

Mambas are fast-moving, highly venomous snakes of the genus Dendroaspis (which literally means "tree asp") in the family Elapidae. Four extant species are recognized currently; three of those four species are essentially arboreal and green in colour, whereas the black mamba, Dendroaspis polylepis, is largely terrestrial and generally brown or grey in colour. All are native to various regions in sub-Saharan Africa and all are feared throughout their ranges, especially the black mamba. In Africa there are many legends and stories about mambas.

Tramadol, sold under the brand name Tramal among others, is an opioid pain medication and a serotonin–norepinephrine reuptake inhibitor (SNRI) used to treat moderate to severe pain. When taken by mouth in an immediate-release formulation, the onset of pain relief usually begins within an hour. It is also available by injection. It is available in combination with paracetamol (acetaminophen).

Pethidine, also known as meperidine and sold under the brand name Demerol among others, is a fully synthetic opioid pain medication of the phenylpiperidine class. Synthesized in 1938 as a potential anticholinergic agent by the German chemist Otto Eisleb, its analgesic properties were first recognized by Otto Schaumann while working for IG Farben, in Germany. Pethidine is the prototype of a large family of analgesics including the pethidine 4-phenylpiperidines (e.g., piminodine, anileridine), the prodines (e.g., alphaprodine, MPPP), bemidones (e.g., ketobemidone), and others more distant, inclu

Clomipramine, sold under the brand name Anafranil among others, is a tricyclic antidepressant (TCA). It is used in the treatment of various conditions, most notably obsessive–compulsive disorder but also many other disorders, including hyperacusis, panic disorder, major depressive disorder, trichotillomania, body dysmorphic disorder and chronic pain. It has also been notably used to treat premature ejaculation and the cataplexy associated with narcolepsy.

Paroxetine, sold under the brand name Paxil among others, is an antidepressant medication of the selective serotonin reuptake inhibitor (SSRI) class used to treat major depressive disorder, obsessive–compulsive disorder (OCD), panic disorder, social anxiety disorder, post-traumatic stress disorder (PTSD), generalized anxiety disorder, and premenstrual dysphoric disorder. It has also been used in the treatment of premature ejaculation, and hot flashes due to menopause. It is taken orally (by mouth).

Chlorphenamine (CP, CPM), also known as chlorpheniramine, is an antihistamine used to treat the symptoms of allergic conditions such as allergic rhinitis (hay fever). It is taken orally (by mouth). The medication takes effect within two hours and lasts for about 4–6 hours. It is a first-generation antihistamine and works by blocking the histamine H1 receptor.

Maprotiline, sold under the brand name Ludiomil among others, is a tetracyclic antidepressant (TeCA) that is used in the treatment of depression. It may alternatively be classified as a tricyclic antidepressant (TCA), specifically a secondary amine. In terms of its chemistry and pharmacology, maprotiline is closely related to such-other secondary-amine TCAs as nortriptyline and protriptyline and has similar effects to them, albeit with more distinct anxiolytic effects. Additionally, whereas protriptyline tends to be somewhat more stimulating and in any case is distinctly more-or-less non-sedat

Trimipramine, sold under the brand name Surmontil among others, is a tricyclic antidepressant (TCA) which is used to treat depression. It has also been used for its sedative, anxiolytic, and weak antipsychotic effects in the treatment of insomnia, anxiety disorders, and psychosis, respectively. The drug is described as an atypical or "second-generation" TCA because, unlike other TCAs, it seems to be a fairly weak monoamine reuptake inhibitor. Similarly to other TCAs, however, trimipramine does have antihistamine, antiserotonergic, antiadrenergic, antidopaminergic, and anticholinergic activitie

thumb|Benzydamine medicinal mouthwash as sold in Argentina. Benzydamine (also known as Tantum Verde and branded in some countries as Maxtra Gargle, Difflam and Septabene), available as the hydrochloride salt, is a locally acting nonsteroidal anti-inflammatory drug (NSAID) with local anaesthetic and analgesic properties for pain relief and anti-inflammatory treatment of inflammatory conditions of the mouth and throat. It falls under class of chemicals known as indazoles.

Amoxapine, sold under the brand name Asendin among others, is a tricyclic antidepressant (TCA). It is the N-demethylated metabolite of loxapine. Amoxapine first received marketing approval in the United States in 1980, approximately 10 to 20 years after most of the other TCAs were introduced in the United States.

Clemastine, also known as meclastin, is a first-generation H1 histamine antagonist (antihistamine) with anticholinergic properties (drying) and sedative side effects. Like all first-generation antihistamines, it is sedating.

Triprolidine is an over-the-counter antihistamine with anticholinergic properties. It is used to combat the symptoms associated with allergies and is sometimes combined with other cold medications designed to provide general relief for flu-like symptoms. As with many antihistamines, the most common side effect is drowsiness.

Pheniramine (trade name Avil among others) is an antihistamine with anticholinergic properties used to treat allergic conditions such as hay fever or urticaria. It has relatively strong sedative effects, and may sometimes be used off-label as an over-the-counter sleeping pill in a similar manner to other sedating antihistamines such as diphenhydramine. Pheniramine is also commonly found in eyedrops used for the treatment of allergic conjunctivitis.

thumb|The toxic berry of Atropa belladonna which contains the tropane deliriants [[scopolamine, atropine, and hyoscyamine.]]

Mepyramine, also known as pyrilamine, is a first-generation antihistamine, targeting the H1 receptor as an inverse agonist. Mepyramine rapidly permeates the brain, often causing drowsiness.

Olopatadine, sold under the brand name Patanol among others, is an antihistamine medication used to decrease the symptoms of allergic conjunctivitis and allergic rhinitis (hay fever). It is used as eye drops or as a nasal spray. The eye drops generally result in an improvement within half an hour.

Brompheniramine, sold under the brand name Dimetapp among others, is a first-generation antihistamine drug of the propylamine (alkylamine) class. It is indicated for the treatment of the symptoms of the common cold and allergic rhinitis, such as runny nose, itchy eyes, watery eyes, and sneezing. Like the other first-generation drugs of its class, it is considered a sedating antihistamine.

Nefopam, sold under the brand name Acupan among others, is a centrally acting, non-opioid analgesic medication, with stimulant and sympathomimetic properties that is primarily used to treat moderate to severe pain.

Protriptyline, sold under the brand name Vivactil among others, is a tricyclic antidepressant (TCA), specifically a secondary amine. Uniquely among most of the TCAs, protriptyline tends to be energizing instead of sedating, and is sometimes used for narcolepsy to achieve a wakefulness-promoting effect.

Buclizine is an antihistamine and anticholinergic of the diphenylmethylpiperazine group. It is considered to be an antiemetic, similar to meclizine.

Dexchlorpheniramine (trade name Polaramine) is an antihistamine with anticholinergic properties used to treat allergic conditions such as hay fever or urticaria. It is the pharmacologically active dextrorotatory isomer of chlorpheniramine.

chemical compound

3-Iodothyronamine (T1AM) is an endogenous thyronamine. It is a high-affinity ligand of the trace amine-associated receptor 1 (TAAR1). T1AM is the most potent endogenous TAAR1 agonist yet discovered. It is also an agonist of the TAAR2 and TAAR5 with similar potency as for the TAAR1 (all in the case of the human proteins). T1AM is not a ligand of the thyroid hormone receptors. However, it is additionally a ligand of various monoamine and other receptors. For instance, it is a muscarinic acetylcholine receptor antagonist.

chemical compound

drug that binds to but does not activate muscarinic cholinergic receptors, thereby blocking the actions of endogenous acetylcholine or exogenous agonists

Revefenacin, sold under the brand name Yupelri, is a medication for the treatment of chronic obstructive pulmonary disease (COPD). It was approved for use in the United States in 2018. It was developed by Theravance Biopharma and is marketed by Mylan. Revefenacin is formulated as a solution that is nebulized and inhaled.

Benactyzine is an anticholinergic drug that was used in the treatment of clinical depression and anxiety disorders before it was pulled from the U.S. market by the FDA due to serious side effects.

Pizotifen, also known as pizotyline and sold under the brand names Sandomigran and Mosegor among others, is an antimigraine agent of the tricyclic group which is used primarily as a preventative to reduce the frequency of recurrent migraine headaches.

chemical compound

Metopimazine (, , ), sold under the brand names Vogalen and Vogalene, is an antiemetic of the phenothiazine group which is used to treat nausea and vomiting. It is marketed in Europe, Canada, and South America. As of August 2020, metopimazine has been repurposed and is additionally under development for use in the United States for the treatment of gastroparesis.

Captodiame (INN), also known as captodiamine, is an antihistamine sold under the trade names Covatine, Covatix, and Suvren which is used as a sedative and anxiolytic. The structure is related to diphenhydramine.

Pridinol, sold under the brand name Myopridin, is a muscle relaxant, anticholinergic and antiparkinsonian drug. It has also been evaluated for the treatment of muscle related pain.

Butriptyline, sold under the brand name Evadyne among others, is a tricyclic antidepressant (TCA) that has been used in the United Kingdom and several other European countries for the treatment of depression but appears to no longer be marketed. Along with trimipramine, iprindole, and amoxapine, it has been described as an "atypical" or "second-generation" TCA due to its relatively late introduction and atypical pharmacology. It was very little-used compared to other TCAs, with the number of prescriptions dispensed only in the thousands.

EA-3167 is a potent and long-lasting anticholinergic deliriant drug, related to the chemical warfare agent 3-quinuclidinyl benzilate (QNB) and to the bronchodilator drug tiotropium bromide. It was developed under contract to Edgewood Arsenal during the 1960s as part of the US military chemical weapons program, in an attempt to develop non-lethal incapacitating agents. EA-3167 has identical effects to QNB (EA-2277), but is even more potent and longer-lasting, with an effective dose when administered by injection of as little as 2.5 μg/kg (i.e. 0.2 milligrams for an 80 kg person), and a dur

Phenindamine (Nolahist, Thephorin) is an antihistamine and anticholinergic closely related to cyproheptadine. It was developed by Hoffman-La Roche in the late 1940s. It is used to treat symptoms of the common cold and allergies, such as sneezing, itching, rashes, and hives. Its efficacy against some symptoms of opioid withdrawal was researched in the 1950s and 1960s in a number of countries; William S. Burroughs' book Junkie mentions this technique. Like many other first-generation antihistamines, phenindamine has useful potentiating effects on many narcotic analgesics and is even more useful

Imipraminoxide (brand names Imiprex, Elepsin), or 'imipramine N-oxide', is a tricyclic antidepressant (TCA) that was introduced in Europe in the 1960s for the treatment of depression.

Isopropamide (R79) is a long-acting anticholinergic drug. It is used in the treatment of peptic ulcers and other gastrointestinal disorders involving hyperacidity (gastrointestinal acidosis) and hypermotility. Chemically, it contains a quaternary ammonium group. It is most often provided as an iodide salt, but is also available as a bromide or chloride salt. It was discovered at Janssen Pharmaceutica in 1954.

combination drug

Imidafenacin (INN) is a urinary antispasmodic of the anticholinergic class. It is used for the treatment of urinary incontinence and related bladder issues, especially in patients with benign prostatic hyperplasia or who have had prostate surgery. Unlike most related drugs, it is orally active but still shows a rapid onset of action, which makes it more convenient to administer.

chemical compound

Nitroxazepine (brand name Sintamil) is a tricyclic antidepressant (TCA) which was introduced by Ciba-Geigy (now Novartis) for the treatment of depression in India in 1982. It is also indicated for the treatment of nocturnal enuresis. Nitroxazepine acts as a serotonin-norepinephrine reuptake inhibitor and has similar effects to imipramine, but with certain advantages, such as lower anticholinergic side effects.

Dexetimide (brand name Tremblex) is a piperidine anticholinergic. It is a muscarinic antagonist that is used to treat drug induced parkinsonism. Dexetimide was discovered at Janssen Pharmaceutica in 1968.

Amitriptylinoxide (brand names Amioxid, Ambivalon, Equilibrin), or 'amitriptyline N-oxide', is a tricyclic antidepressant (TCA) which was introduced in Europe in the 1970s for the treatment of depression.

Pyrrobutamine is an antihistamine and anticholinergic.

Camylofin is an antimuscarinic drug.

Fluacizine, sold under the brand name Phtorazisin, is a tricyclic antidepressant (TCA) of the phenothiazine group which is or was marketed in Russia. Unlike other phenothiazines, fluacizine is not an antipsychotic, and can actually reverse catalepsy and extrapyramidal symptoms induced by antidopaminergic agents like antipsychotics, reserpine, and tetrabenazine as well as potentiate amphetamine-induced stereotypy. It is known to act as a norepinephrine reuptake inhibitor, antihistamine, and anticholinergic. The drug was developed in the 1960s and was marketed in the 1970s. It is the trifluorome

pharmaceutical drug

Tofenacin is an antidepressant drug with a tricyclic-like structure which was developed and marketed in the United Kingdom and Italy in 1971 and 1981, respectively, by Brocades-Stheeman & Pharmacia (now part of Astellas Pharma). It acts as a serotonin-norepinephrine reuptake inhibitor, and based on its close relation to orphenadrine, may also possess anticholinergic and antihistamine properties. Tofenacin is also the major active metabolite of orphenadrine and likely plays a role in its beneficial effects against depressive symptoms seen in Parkinson's disease patients.

Phenglutarimide (brand names Aturbal and Aturbane) is an anticholinergic used as an antiparkinsonian agent.

Oxyphencyclimine is a muscarinic receptor antagonist, given orally to treat peptic ulcer disease and gastrointestinal spasms. It has antispasmodic and antimotility properties.

Anisodine, also known as daturamine and α-hydroxyscopolamine, is an antispasmodic and anticholinergic drug used in the treatment of acute circulatory shock in China. It is a tropane alkaloid and is found naturally in plants of the family Solanaceae - notably Anisodus tanguticus (syn. Scopolia tangutica. Anisodine acts as a muscarinic acetylcholine receptor antagonist and α1-adrenergic receptor antagonist.

Dihexyverine is an anticholinergic spasmolytic. It is not approved for use in the United States but is sold in France under the trade name Spasmodex.

Rociverine is an antispasmodic drug used to treat urinary, gastrointestinal and biliary spasms. It is antimuscarinic drug.

Anisodamine, also known as '7β-hydroxyhyoscyamine, is a mAChR anticholinergic and α1 adrenergic receptor antagonist used in the treatment of acute circulatory shock in China. It is given orally or by injection, as a racemic mixture (racanisodamine') or as a hydrobromide salt of the natural enantiometer. Eye drops at 0.5% concentration for slowing the progression of myopia is also available in China.

Methantheline is an antimuscarinic.

Hydroxyethylpromethazine is an antihistamine with anticholinergic properties. It is structurally analogous to promethazine.

Poldine is an antimuscarinic that is used to treat peptic ulcers.

Profenamine (INN; also known as ethopropazine (BAN); sold under the trade name Parsidol and others) is a phenothiazine derivative used as an antiparkinsonian agent that has anticholinergic, antihistamine, and antiadrenergic actions. It is also used in the alleviation of the extrapyramidal syndrome induced by drugs such as other phenothiazine compounds, but, like other compounds with antimuscarinic properties, is of no value against tardive dyskinesia.

chemical compound