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Cholinergic Antagonists: (Cholinergic blockers or anticholinergic drugs)
They block the various types of cholinergic receptors. Antimuscarinic Drugs:
They block the action of Acetylcholine at muscarinic receptors and also effects of parasympathetic nerve stimulation.
Ganglion Blocking drugs:
They block the action of Acetylcholine at autonomic ganglia. (Nicotinic receptors).
Neuromuscular blocking drugs:
They block the effect of Acetylcholine at N.M junction.
y Antimuscarinic drugs include naturally occuring Belladonna Alkaloids (Atropine.Antimuscarinic Drugs y They are also called Parasympatholytic drugs Or Anticholinergics. . Hyoscine) and a large number of semisynthetic and synthetic drugs. where higher concentrations of antagonist are required. y They reduce or abolish (block) the muscarinic receptor mediated effects of parasympathetic nervous system. The dosed required to block the responses to parasympathetic stimulation are greater than those required to block effects of exogenously administered drugs. It is due to the fact that by nerve stimulation the acetylcholine is liberated very close to the receptors.
Classification: y Natural alkaloids: y Spasmolytics Atropine y Hyoscine y Semisynthetic compounds: y Atropine methonitrate y Hyoscine methobromide y Hyoscine butylbromide y Homatropine methylbromide y Synthetic compounds: y y Mydriatic and Cycloplegics: y y y (antispasmodics) y y y y y y Propantheline Isopropamide Ipratropium (anti asthmatics) Glycopyrrolate Pirenzepine Dicyclomine Trihexyphenidyl Benztropine Biperiden y Anti-Parkinsonism Agents: y y y Cyclopentolate Tropicamide Homatropine .
such as those innervating sweat glands. for example atropine and hyoscine. block muscarinic receptors. y ATROPINE (Prototype) Source Plant Atropa Belladonna Datura stramonium Atropa Acuminata Hyoscyamus niger Scopolia Carniolica Alkaloid Atropine Atropine Atropine Hyoscine Hyoscine .ANTIMUSCARINIC DRUGS y These drugs. In addition these drugs block the sympathetic neurons that are cholinergic.
scopine. . The action of atropine is reversible and can be overcome by increasing the concentration of acetylcholine or any other muscarinic agonist or by the use of anticholinesterase. tropine.Atropine y Chemistry: Atropine is an alkaloid ester of tropic acid with an organic base. y Mechanism of Action: Atropine is a competitive antagonist of acetylcholine at muscarinic receptors. Hyoscine is an ester of tropic acid with an organic base.
. Its halflife is about 4 hrs. About half of the dose is secreted unchanged in urine.Atropine y Pharmacokinetics: Atropine is lipid soluble. and is secreted in milk. It is metabolized in liver. Rapidly absorbed from GIT and mucous membranes (conjunctiva). It can cross BBB (Blood-Brain Barrier) and placental barrier.
Effects of atropine can occur after local or systemic administration. the lens becomes flat and fixed for far (distant) vision. This is called cycloplegia. y In elderly patients with shallow anterior chamber. the mydriatic effect remains for 5-7 days and cycloplegic action for 6-10 days. Light reflex is abolished and this caused photophobia. atropine can precipitate acute congestive glaucoma. The unopposed action of dilator pupillae (radial) muscles causes mydriasis . y The ciliary muscle is relaxed with paralysis (loss) of accommodation. causing their relaxation.Atropine y Pharmacological Actions y Eye: Atropine blocks muscarinic receptors of circular muscles. After applying locally. y There is increase in the intra-ocular pressure because the iris crowded back into the anterior chamber of the eye interferes with the drainage of aqueous humor. .
Mouth becomes dry and swallowing becomes difficult. y Pirenzepine . Gastric secretion is reduced in volume but H+ concentration remains unaltered. Its motor activity is inhibited.Atropine y Gastrointestinal Tract: y Atropine markedly reduces salivary secretions. does reduce gastric acid secretion in doses that do not antagonize other systems. . There is decrease in the tone as well as amplitude and frequency of peristaltic contractions. y Atropine markedly reduces motility of the GIT. a M1 muscarinic antagonist.
Atropine y Gall Bladder: y Atropine has a mild antispasmodic effect on bile ducts and gall bladder. It causes urinary retention especially in elderly males with enlarged prostate. Detrusor muscle is relaxed and sphincter contracts. . y Urinary Tract: y Atropine decreases tone and amplitude of contractions of ureter and urinary bladder. but it cannot overcome the spasm of bile ducts induced by morphine.
y Atropine causes bronchodilatation resulting in increase in the rate and depth of respiration. It reduces the secretions of the respiratory tract and hence it is used a preanesthetic medication.Atropine y Respiratory Tract: y Atropine acts on the bronchial glands and bronchial smooth muscles. y Ipratropium bromide. . a synthetic quaternary antimuscarinic compound is being used by inhalation.
This initial bradycardia occurs due to: y Transient initial stimulation of dorsal nucleus of Vagus Nerve. It causes transient bradycardia. . y Blockade of pre-synaptic M1 receptors on postganglionic parasympathetic neurons.Atropine y Cardiovascular System: y Atropine has a biphasic action on the heart. especially noticeable at low doses.
Atropine is used as pre-anesthetic medication as it may prevent excessive vagal slowing of the heart during anesthesia. y Does not affect blood pressure unless there is hypotension as a result of bradycardia e.in which case atropine may return the pressure to a normal value y In large doses there may be dilatation of cutaneous blood vessels (atropine flush) in face and neck. y Large doses causes tachycardia due to blockade of cardiac M2.Continued . unrelated to cholinergic innervation. .receptors on SA node and AV node.g following acute myocardial infarction. which may be due to direct action.
and delirium. there is rise in the body temperature. Large doses cause restlessness. These are blocked by atropine resulting in no sweating and no heat loss. y Central Nervous System: Atropine stimulates CNS. . Infants and small children are more sensitive to this effect and suffer from Atropine fever.Atropine y Sweat Glands: y Sweat gland of the skin are innervated by sympathetic cholinergic fibers. irritability. hallucinations. Stimulation is followed by depression. Atropine reduces tremors and rigidity in Parkinsonism. which play an important role in thermoregulation. where there is cholinergic activity.
It is used in peptic ulcer. y Hyoscine Butylbromide: y It is used for esophageal and gastrointestinal spastic conditions. spasm of ureter and bile duct. It is used in congenital hypertrophic pyloric stenosis and pylorospasm in children. bile duct and ureter. peptic ulcer. y Homatropine Methylbromide: y Used topically as mydriatic and cycloplegic. . renal colic and cystitis.Semisynthetic Derivatives y Atropine Methonitrate: y It is a quaternary derivative of atropine. It is also used orally to treat the spasm of GIT. y Hyoscine Methobromide: y It is a quaternary derivative of hyoscine.
cross Blood-Brain barrier and act on the basal ganglia. Given orally. So it can be used in chronic obstructive pulmonary diseases (COPD). Used for gastrointestinal and genitourinary conditions. pylorospasm and gastric secretion. y Ipratropium Bromide y It is used as a bronchodilator. by inhalation.Spasmolytics: y They are quaternary ammonium compounds. It is selective antagonist of M1 receptors. y Antiparkinsonism Agents y Have weak peripheral anticholinergic action. which are present in the intra-mural plexus of the stomach and reduced gastric secretions without interference with M2 receptor. . They reduce gastric motility. y Pirenzepine y It is a tertiary amine. It is used in the treatment of peptic ulcer. It does not interfere with the functions of ciliated epithelium of bronchial tree.
Longer acting drugs like atropine may be used alternately with a miotic agent to break the adhesions in uveitis and iritis.THERAPEUTIC USES OF ANTIMUSCARINIC DRUGS y Eye Conditions: y Antimuscarinic drugs are used to produce mydriasis and cycloplegia. a sympathomimetic drug like phenylephrine is used.for accurate measurement of refractive errors . When only mydriasis is required. y Also used topically for thorough examination of retina and optic disk.
y Central Nervous system y Parkinsonism y Motion sickness hyoscine butyl bromide prophylactically .Continued uses y Gastrointestinal System: y y Antisecretory: Used in peptic ulcer Antispasmodic: used in intestinal colic. incontinence of urine. cystitis. biliary colic y Genitourinary System: y Used in ureteric colic. (nocturnal enuresis).
. y Cardiovascular and respiratory system: y Preanesthetic medication: useful in preventing: y y Increased secretions of respiratory tract due to irritant effects of anesthesia..Uses continued. y Extreme bradycardia associated with: -Acute M. Vagal effects of some anesthetics y Bronchial asthma: Ipratropium is used by inhalation.I in whom excessive vagal tone causes sinus or nodal bradycardia -A V block .
. In treatment of mushroom poisoning. To antagonize the muscarinic effects of neostigmine.Uses continued y y y In the treatment of organophosphorus compound Poisoning.
delay in gastric emptying-time will expose the ulcer to acid for longer time. y In patients with gastric ulcer. y In patients with enlarges prostate there may be retention of urine. with shallow anterior chamber.Precautions with Atropine-like drugs y In patients over 40 years of age. systemic or topical administration of these drugs may precipitate acute congestive glaucoma. if it is given alone. . y In coronary artery disease atropine may precipitate angina. it may result in complete stenosis. y In patients with partial pyloric stenosis.
pupils dilated. Atropine flush(face and neck) y Palpitations y Dysuria. dysphagia. photophobia.Poisoning of Antimuscarinic Drugs y Symptoms and signs: They are due to peripheral blockade of muscarinic receptors and the actions on CNS. . y hyperpyrexia(atropine fever most dangerous). retention of urine. hot. scarlet rash may appear. y Peripheral muscarinic effects: y Dry mouth. loss of accommodation. thirst. y Skin Dry. constipation.
salivation. hallucinations. y red as a beet. sweating . disorientation.lacrimation.all reduced y blind as a bat. y mad as a hatter . y Dry as a bone(bec. This is followed by depression of vasomotor center and respiratory center.y Central nervous system effects: y They are: y Excitement. restlessness. delirium.
Specific treatment(Antidote) Physostigmine I/V. Removal of unabsorbed drug by gastric lavage with KMnO4 or activated charcoal. To counteract excitement and convulsions diazepam. oxygen. artificial respiration. .Treatment y y y y Treatment of hyperpyrexia ice bag.
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