Also called cholinoceptor antagonist, they have the ability to bind to the receptors of acetylcholine, either muscarinic or nicotinic receptors, and prevent the binding of acetylcholine and other agonists
Cholinoceptor antagonists
They only have the ability to bind to the receptor with high affinity but they don't have intrinsic activity, they are not capable of activating the receptors
Muscarinic receptor blocking drugs
Also called anticholinergic agents or parasympatholytics, they specifically antagonise muscarinic receptors without activating them
Muscarinic receptor antagonists
Atropine
Hyoscyamine
Atropine
The prototype muscarinic receptor antagonist, also called hyoscyamine, derived from plants like Atropa belladonna, Datura stramonium, and Datura metel
Mechanism of action of atropine
Binds to and blocks muscarinic receptors, thereby preventing the effects of acetylcholine and other cholinergic agonists
Effects of atropine
Dilates pupils (mydriasis)
Causes cycloplegia (loss of accommodation)
Reduces lacrimation (dry eyes)
Reduces gastrointestinal secretions and motility (dry mouth, prolonged gastric emptying)
Increases heart rate (at low doses, can cause tachycardia at high doses)
Causes bronchodilation
Causes urinary retention
Antispasmodic drugs
Drugs that can relieve smooth muscle spasms, e.g. atropine, hyoscine and butylbromide (Buscopan)
Atropine and Buscopan (hyoscine and butylbromide) are used to treat intestinal spasms
Atropine can have adverse effects like intestinal paralysis if overdosed
Irregular menstrual cycles can be due to hormonal imbalances, and can be improved through diet and exercise
The calendar method for contraception is not reliable for women with irregular cycles
Depo-Provera is a contraceptive injection containing a hormone that can affect the menstrual cycle
Loperamide
An anticholinergic drug used to treat diarrhea, often combined with atropine (Lomotil)
At low doses, atropine can cause bradycardia
At high doses, it can cause tachycardia
Atropine can cause bronchodilation, which is useful for asthma and COPD patients
Atropine can cause urinary retention, which can be beneficial for patients with incontinence
Atropine can reduce sweating, but should be used cautiously in infants with fever
Bradycardia
Slow heart rate
Bronchoconstriction
Narrowing of the airways
Bronchodilation
Widening of the airways
Atropine and other anticholinergics cause bronchodilation, which is a useful effect for patients with asthma and COPD
Urinary retention
Inability to urinate
Urinary incontinence
Involuntary voiding
Atropine can cause urinary retention, which is beneficial, but not for patients with hyperhidrosis (excessive sweating)
Atropine is not effective for treating hyperhidrosis because the apocrine glands, not the eccrine glands, are responsible for excessive sweating
Atropine at normal doses causes stimulation of the central nervous system, which is why it is a prescription drug
Atropine at higher doses has a sedative effect on the central nervous system
Atropine
It is a mydriatic drug (dilates the pupils)
It is a cycloplegic agent (weakens the muscles of accommodation in the eye, causing loss of near vision focus)
Atropine
It has antispasmodic effects, relaxing smooth muscles in the gastrointestinal tract
It can increase heart rate (tachycardia) at high doses
Atropine is included in emergency kits in hospitals and is highly monitored by pharmacists
Atropine is used for treating cholinergic agonist poisoning, such as from organophosphate insecticides
Adverse effects of atropine
Blurred vision
Dry mouth
Tachycardia
Urinary retention
Constipation
Restlessness
Confusion
Delirium
Hallucinations
Atropine is contraindicated in people with prostatic hyperplasia (enlarged prostate)
Scopolamine
Also known as hyoscine, it is another anticholinergic alkaloid
Scopolamine
It has greater effects on the central nervous system compared to atropine
It is an effective anti-motion sickness drug
It can cause sedation and short-term memory impairment
Ipratropium
A synthetic anticholinergic drug used for asthma and COPD
Ipratropium is the only anticholinergic drug used for asthma and COPD
Tiotropium
A newer once-daily anticholinergic drug for asthma and COPD
Oxybutynin
An anticholinergic drug used for bladder spasms and urinary incontinence