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  • Cholinergic antagonist

    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