Muscarinic antagonist
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Muscarinic acetylcholine receptor antagonist | |
---|---|
Drug class | |
![]() Skeletal formula of scopolamine, a nonselective antagonist of the muscarinic receptors | |
Class identifiers | |
Use | Allergies, asthma, atrial fibrillation with bradycardia,[1] motion sickness, Parkinson's disease, etc. |
ATC code | V |
Biological target | Metabotropic acetylcholinergic receptors |
External links | |
MeSH | D018727 |
Legal status | |
In Wikidata |
A muscarinic receptor antagonist (MRA), also called an antimuscarinic, is a type of anticholinergic agent that blocks the activity of the muscarinic acetylcholine receptor. The muscarinic receptor is a protein involved in the transmission of signals through certain parts of the nervous system, and muscarinic receptor antagonists work to prevent this transmission from occurring. Notably, muscarinic antagonists reduce the activation of the parasympathetic nervous system. The normal function of the parasympathetic system is often summarised as "rest-and-digest", and includes slowing of the heart, an increased rate of digestion, narrowing of the airways, promotion of urination, and sexual arousal. Muscarinic antagonists counter this parasympathetic "rest-and-digest" response, and also work elsewhere in both the central and peripheral nervous systems.
Drugs with muscarinic antagonist activity are widely used in medicine, in the treatment of low heart rate, overactive bladder, respiratory problems such as asthma and chronic obstructive pulmonary disease (COPD), and neurological problems such as Parkinson's disease and Alzheimer's disease. A number of other drugs, such as antipsychotics and the tricyclic family of antidepressants, have incidental muscarinic antagonist activity which can cause unwanted side effects such as difficulty urinating, dry mouth and skin, and constipation.
Acetylcholine (often abbreviated ACh) is a neurotransmitter whose receptors are proteins found in synapses and other cell membranes. Besides responding to their primary neurochemical, neurotransmitter receptors can be sensitive to a variety of other molecules. Acetylcholine receptors are classified into two groups based on this:
Most muscarinic receptor antagonists are synthetic chemicals; however, the two most commonly used anticholinergics, scopolamine and atropine, are belladonna alkaloids, and are naturally extracted from plants such as Atropa belladonna, the deadly nightshade. The name "belladonna", Italian for "beautiful lady", is thought to derive from one of the antimuscarinic effects of these alkaloids: they were used by women for cosmetic purposes, to promote dilation of the pupils.[2]
Muscarinic antagonist effects and muscarinic agonist effects counterbalance each other for homeostasis.
Certain muscarinic antagonists can be classified into either long-acting muscarinic receptor antagonists (LAMAs) or short-acting muscarinic receptor antagonists (SAMAs), depending on when maximum effect occurs and for how long the effect persists.[3]
Effects
[edit]This section needs additional citations for verification. (March 2024) |
Scopolamine and atropine have similar effects on the peripheral nervous system. However, scopolamine has greater effects on the central nervous system (CNS) than atropine due to its ability to cross the blood–brain barrier.[4] At higher-than-therapeutic doses, atropine and scopolamine cause CNS depression characterized by amnesia, fatigue, and reduction in rapid eye movement sleep. Scopolamine (Hyoscine) has anti-emetic activity and is, therefore, used to treat motion sickness.
Antimuscarinics are also used as anti-parkinsonian drugs. In parkinsonism, there is imbalance between levels of acetylcholine and dopamine in the brain, involving both increased levels of acetylcholine and degeneration of dopaminergic pathways (nigrostriatal pathway). Thus, in parkinsonism there is decreased level of dopaminergic activity. One method of balancing the neurotransmitters is through blocking central cholinergic activity using muscarinic receptor antagonists.
Atropine acts on the M2 receptors of the heart and antagonizes the activity of acetylcholine. It causes tachycardia by blocking vagal effects on the sinoatrial node. Acetylcholine hyperpolarizes the sinoatrial node; this is overcome by MRAs, and thus they increase the heart rate. If atropine is given by intramuscular or subcutaneous injection, it causes initial bradycardia. This is because when administered intramuscularly or subcutaneously atropine acts on presynaptic M1 receptors (autoreceptors). Uptake of acetylcholine in axoplasm is prevented and the presynaptic nerve releases more acetylcholine into the synapse, which initially causes bradycardia.
In the atrioventricular node, the resting potential is lowered, which facilitates conduction. This is seen as a shortened PR-interval on an electrocardiogram. It[clarification needed] has an opposite effect on blood pressure. Tachycardia and stimulation of the vasomotor center causes an increase in blood pressure. But, due to feedback regulation of the vasomotor center, there is a fall in blood pressure due to vasodilation.
Important[5] muscarinic antagonists include atropine, hyoscyamine, hyoscine butylbromide and hydrobromide, ipratropium, tropicamide, cyclopentolate, pirenzepine and scopalamine.
Muscarinic antagonists such as ipratropium bromide can also be effective in treating asthma, since acetylcholine is known to cause smooth muscle contraction, especially in the bronchi.
Comparison table
[edit]![]() |
Overview
[edit]Substance | Selectivity | Clinical use | Adverse effects | Notes | Trade names |
---|---|---|---|---|---|
Atropine (D/L-Hyoscyamine) | NS |
| CD[5] | Symax, HyoMax, Anaspaz, Egazil, Buwecon, Cystospaz, Levsin, Levbid, Levsinex, Donnamar, NuLev, Spacol T/S and Neoquess | |
Atropine methonitrate | NS |
| Blocks transmission in ganglia.[5] Lacks CNS effects[7] | ||
Aclidinium bromide | Selective[clarification needed] |
| Long acting antagonist | Tudorza | |
Benztropine | M1-selective |
| Reduces the effects of the relative central cholinergic excess that occurs as a result of dopamine deficiency. | Cogentin | |
Cyclopentolate | NS |
|
| Short acting, CD[5] | |
Diphenhydramine | NS |
|
| Acts in the central nervous system, blood vessels and smooth muscle tissues | Benadryl, Nytol |
Doxylamine | NS |
|
| Unisom | |
Dimenhydrinate | Combination of diphenhydramine with a methylxanthine salt | Dramamine, Gravol | |||
Dicyclomine | Bentyl | ||||
Darifenacin | Selective for M3[7] | Urinary incontinence [7] | Few side effects[7] | Enablex | |
Flavoxate | Urispas | ||||
Glycopyrrolate (Glycopyrronium bromide) | NS |
| Does not cross the blood–brain barrier and has few to no central effects.[9] | Robinul, Cuvposa, Seebri | |
Hydroxyzine | Very mild/negligible action | Vistaril, Atarax | |||
Ipratropium bromide | NS | Asthma and bronchitis[5] |
| Lacks mucociliary excretion inhibition.[5] | Atrovent and Apovent |
Mebeverine |
|
| A muscolotropic spasmolytic with a strong and selective action on the smooth muscle spasm of the gastrointestinal tract, in particular of the colon. | Colofac, Duspatal, Duspatalin | |
Oxybutynin | M1/3/4 selective | Ditropan | |||
Pirenzepine | M1-selective[5] |
| (fewer than non-selective ones)[5] | Inhibits gastric secretion[5] | |
Procyclidine | NS |
| Overdose produces confusion, agitation and sleeplessness that can last up to or more than 24 hours. Pupils become dilated and unreactive to light. Tachycardia (fast heart beat), as well as auditory and visual hallucinations | ||
Scopolamine (L-Hyoscine) | NS |
| CD[5] | Scopace, Transderm-Scop, Maldemar, Buscopan | |
Solifenacin |
| Competitive antagonist | Vesicare | ||
Tropicamide | NS |
|
| Short acting, CD[5] | |
Tiotropium | Spiriva | ||||
Trihexyphenidyl/Benzhexol | M1 selective | PD | Drug at relative dose has 83% activity of atropine, thus has the same side-effects | Artane | |
Tolterodine | Detrusitol, Detrol |
Binding affinities
[edit]Anticholinergics
[edit]Compound | M1 | M2 | M3 | M4 | M5 | Species | Ref |
---|---|---|---|---|---|---|---|
3-Quinuclidinyl benzilate | 0.035–0.044 | 0.027–0.030 | 0.080–0.088 | 0.034–0.037 | 0.043–0.065 | Human | [10][11] |
4-DAMP | 0.57–0.58 | 3.80–7.3 | 0.37–0.52 | 0.72–1.17 | 0.55–1.05 | Human | [12][13] |
AF-DX 250 | 427 | 55.0 | 692 | 162 | 3020 | Human | [12] |
AF-DX 384 | 30.9 | 6.03 | 66.1 | 10.0 | 537 | Human | [12] |
AQ-RA 741 | 28.8 | 4.27 | 63.1 | 6.46 | 832 | Human | [12] |
Atropine | 0.21–0.50 | 0.76–1.5 | 0.15–1.1 | 0.13–0.6 | 0.21–1.7 | Human | [10][14][13] |
Benzatropine (benztropine) | 0.231 | 1.4 | 1.1 | 1.1 | 2.8 | Human | [10] |
Biperiden | 0.48 | 6.3 | 3.9 | 2.4 | 6.3 | Human | [10] |
Darifenacin | 5.5–13 | 47–77 | 0.84–2.0 | 8.6–22 | 2.3–5.4 | Human | [13][15] |
Dicycloverine (dicyclomine) | 57 (IC50) | 415 (IC50) | 67 (IC50) | 97 (IC50) | 53 (IC50) | Human/rat | [14] |
Glycopyrrolate | 0.37 | 1.38 | 1.31 | 0.41 | 1.30 | Human | [9] |
Hexahydrodifenidol | 11 | 200 | 16 | 76 (IC50) | 83 | Human/rat | [14] |
Hexahydrosiladifenidol | 44 | 249 | 10 | 298 (IC50) | 63 | Human/rat | [14] |
(R)-Hexbutinol | 2.09 | 20.9 | 2.14 | 3.02 | 5.50 | Human | [12] |
Hexocyclium | 2.3 | 23 | 1.4 | 5.5 | 3.7 | Human/rat | [14] |
Himbacine | 107 | 10.0 | 93.3 | 11.0 | 490 | Human | [12] |
Ipratropium | 0.49 | 1.5 | 0.51 | 0.66 | 1.7 | Human | [15] |
Methoctramine | 16–50 | 3.6–14.4 | 118–277 | 31.6–38.0 | 57–313 | Human | [14][12][16] |
N-Methylscopolamine | 0.054–0.079 | 0.083–0.251 | 0.052–0.099 | 0.026–0.097 | 0.106–0.125 | Human | [12] |
Orphenadrine | 48 | 213 | 120 | 170 | 129 | Human | [11] |
Otenzepad (AF-DX 116) | 1300 | 186 | 838 | 1800 (IC50) | 2800 | Human/rat | [14] |
Oxybutynin | 0.66 | 13 | 0.72 | 0.54 | 7.4 | Human | [13] |
pFHHSiD | 22.4 | 132 | 15.5 | 31.6 | 93.3 | Human | [12] |
Pirenzepine | 6.3–8 | 224–906 | 75–180 | 17–37 | 66–170 | Human | [10][14][12][13] |
Procyclidine | 4.6 | 25 | 12.4 | 7 | 24 | Human | [10] |
Propiverine | 476 | 2970 | 420 | 536 | 109 | Human | [13] |
Scopolamine (hyoscine) | 1.1 | 2.0 | 0.44 | 0.8 | 2.07 | Human | [10] |
Silahexacyclium | 2.0 | 35 | 1.2 | 3.2 | 2.0 | Human/rat | [14] |
Timepidium | 34 | 7.7 | 31 | 18 | 11 | Human | [13] |
Tiquizium | 4.1 | 4.0 | 2.8 | 3.6 | 8.2 | Human | [13] |
Trihexyphenidyl | 1.6 | 7 | 6.4 | 2.6 | 15.9 | Human | [10] |
Tripitamine (tripitramine) | 1.58 | 0.27 | 38.25 | 6.41 | 33.87 | Human | [16] |
Zamifenacin | 55 | 153 | 10 | 68 | 34 | Human | [13] |
Values are Ki (nM). The smaller the value, the more strongly the drug binds to the site. |
Antihistamines
[edit]Compound | M1 | M2 | M3 | M4 | M5 | Species | Ref |
---|---|---|---|---|---|---|---|
Brompheniramine | 25700 | 32400 | 50100 | 67600 | 28800 | Human | [17] |
Chlorphenamine (chlorpheniramine) | 19000 | 17000 | 52500 | 77600 | 28200 | Human | [17] |
Cyproheptadine | 12 | 7 | 12 | 8 | 11.8 | Human | [11] |
Diphenhydramine | 80–100 | 120–490 | 84–229 | 53–112 | 30–260 | Human | [10][18] |
Doxylamine | 490 | 2100 | 650 | 380 | 180 | Human | [18] |
Mequitazine | 5.6 | 14 | 5.3 | 11.1 | 11.0 | Human | [11] |
Terfenadine | 8710 | 8510 | 5250 | 30900 | 11200 | Human | [17] |
Values are Ki (nM). The smaller the value, the more strongly the drug binds to the site. |
Antidepressants
[edit]Compound | M1 | M2 | M3 | M4 | M5 | Species | Ref |
---|---|---|---|---|---|---|---|
Amitriptyline | 14.7 | 11.8 | 12.8 | 7.2 | 15.7 | Human | [11] |
Bupropion | >35,000 | >35,000 | >35,000 | >35,000 | >35,000 | Human | [11] |
Citalopram | 1430 | ND | ND | ND | ND | Human | [19] |
Desipramine | 110 | 540 | 210 | 160 | 143 | Human | [11] |
Desmethylcitalopram | >10000 | >10000 | >10000 | >10000 | >10000 | Human | [20] |
Desmethyldesipramine | 404 | 927 | 317 | 629 | 121 | Human | [20] |
Desvenlafaxine | >10000 | >10000 | >10000 | >10000 | >10000 | Human | [21] |
Dosulepin (dothiepin) | 18 | 109 | 38 | 61 | 92 | Human | [11] |
Doxepin | 18–38 | 160–230 | 25–52 | 20–82 | 5.6–75 | Human | [18][11] |
Escitalopram | 1242 | ND | ND | ND | ND | Human | [19] |
Etoperidone | >35000 | >35000 | >35000 | >35000 | >35000 | Human | [11] |
Femoxetine | 92 | 150 | 220 | 470 | 400 | Human | [11] |
Fluoxetine | 702–1030 | 2700 | 1000 | 2900 | 2700 | Human | [11][19] |
Fluvoxamine | 31200 | ND | ND | ND | ND | Human | [19] |
Imipramine | 42 | 88 | 60 | 112 | 83 | Human | [11] |
Lofepramine | 67 | 330 | 130 | 340 | 460 | Human | [11] |
Norfluoxetine | 1200 | 4600 | 760 | 2600 | 2200 | Human | [11] |
Nortriptyline | 40 | 110 | 50 | 84 | 97 | Human | [11] |
Paroxetine | 72–300 | 340 | 80 | 320 | 650 | Human | [11][19] |
Sertraline | 427–1300 | 2100 | 1300 | 1400 | 1900 | Human | [11][19] |
Tianeptine | >10000 | >10000 | >10000 | >10000 | >10000 | Human | [22] |
Trazodone | >35,000 | >35,000 | >35,000 | >35,000 | >35,000 | Human | [18][11] |
Venlafaxine | >35000 | >35000 | >35000 | >35000 | >35000 | Human | [11] |
Values are Ki (nM). The smaller the value, the more strongly the drug binds to the site. |
Antipsychotics
[edit]Compound | M1 | M2 | M3 | M4 | M5 | Species | Ref |
---|---|---|---|---|---|---|---|
Amisulpride | >10,000 | >10,000 | >10,000 | >10,000 | >10,000 | Human | [23] |
Aripiprazole | 6780 | 3510 | 4680 | 1520 | 2330 | Human | [24] |
Asenapine | >10000 | >10000 | >10000 | >10000 | ND | Human | [25] |
Bromperidol | 7600 | 1800 | 7140 | 1700 | 4800 | Human | [10] |
Chlorprothixene | 11 | 28 | 22 | 18 | 25 | Human | [10] |
Chlorpromazine | 25 | 150 | 67 | 40 | 42 | Human | [10] |
Clozapine | 1.4–31 | 7–204 | 6–109 | 5–27 | 5–26 | Human | [10][25][26][27] |
Cyamemazine (cyamepromazine) | 13 | 42 | 32 | 12 | 35 | Human | [28] |
N-Desmethylclozapine | 67.6 | 414.5 | 95.7 | 169.9 | 35.4 | Human | [29] |
Fluperlapine | 8.8 | 71 | 41 | 14 | 17 | Human | [10] |
Fluphenazine | 1095 | 7163 | 1441 | 5321 | 357 | Human | [30] |
Haloperidol | >10000 | >10000 | >10000 | >10000 | >10000 | Human | [25][26] |
Iloperidone | 4898 | 3311 | >10000 | 8318 | >10000 | Human | [31] |
Loxapine | 63.9–175 | 300–590 | 122–390 | 300–2232 | 91–241 | Human | [10][32] |
Melperone | >15000 | 2400 | >15000 | 4400 | >15000 | Human | [10] |
Mesoridazine | 10 | 15 | 90 | 19 | 60 | Human | [10] |
Molindone | ND | ND | >10000 | ND | ND | Human | [33] |
Olanzapine | 1.9–73 | 18–96 | 13–132 | 10–32 | 6–48 | Human | [25][26][27] |
Perphenazine | ND | ND | 1848 | ND | ND | Human | [33] |
Pimozide | ND | ND | 1955 | ND | ND | Human | [33] |
Quetiapine | 120–135 | 630–705 | 225–1320 | 660–2990 | 2990 | Human | [25][26] |
Remoxipride | >10000 | >10000 | >10000 | >10000 | ND | Human | [25] |
Rilapine | 190 | 470 | 1400 | 1000 | 1100 | Human | [10] |
Risperidone | 11000 | ≥3700 | 13000 | ≥2900 | >15000 | Human | [10][25] |
Sertindole | ND | ND | 2692 | ND | ND | Human | [33] |
Tenilapine | 260 | 62 | 530 | 430 | 660 | Human | [10] |
Thioridazine | 2.7 | 14 | 15 | 9 | 13 | Human | [10] |
Thiothixene | >10000 | >10000 | >10000 | >10000 | 5376 | Human | [34] |
cis-Thiothixene | 2600 | 2100 | 1600 | 1540 | 4310 | Human | [10] |
Tiospirone | 630 | 180 | 1290 | 480 | 3900 | Human | [10] |
Trifluoperazine | ND | ND | 1001 | ND | ND | Human | [33] |
Ziprasidone | ≥300 | >3000 | >1300 | >1600 | >1600 | Human | [26][35] |
Zotepine | 18 | 140 | 73 | 77 | 260 | Human | [10] |
Values are Ki (nM). The smaller the value, the more strongly the drug binds to the site. |
See also
[edit]References
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- ^ a b c d e Kroeze WK, Hufeisen SJ, Popadak BA, Renock SM, Steinberg S, Ernsberger P, Jayathilake K, Meltzer HY, Roth BL (2003). "H1-histamine receptor affinity predicts short-term weight gain for typical and atypical antipsychotic drugs". Neuropsychopharmacology. 28 (3): 519–26. doi:10.1038/sj.npp.1300027. PMID 12629531.
- ^ Roth, BL; Driscol, J. "PDSP Ki Database". Psychoactive Drug Screening Program (PDSP). University of North Carolina at Chapel Hill and the United States National Institute of Mental Health. Retrieved 14 August 2017.
- ^ Roth, BL; Driscol, J. "PDSP Ki Database". Psychoactive Drug Screening Program (PDSP). University of North Carolina at Chapel Hill and the United States National Institute of Mental Health. Retrieved 14 August 2017.
External links
[edit]- Effects of Muscarinic Antagonist
- Atropine (Muscarinic Receptor Antagonist), Cardiovascular Pharmacology Concepts, Richard E. Klabunde, PhD
- Muscarinic+antagonists at the U.S. National Library of Medicine Medical Subject Headings (MeSH)
- MeSH list of agents 82018727