PILOCARPINE:

 It is a directly acting parasympathomimetic.

 It is a natural alkaloid.
 It is obtained from the leaves of Pilocarpus microphyllus
PK:
 Tertiary amine.
 Can cross BBB.
Target:
 Muscarinic receptors
Effects:
 It has prominent muscarinic actions and also stimulates ganglia
 Pilocarpine causes marked sweating, salivation and increase in other secretions.
 Small doses generally cause fall in BP (muscarinic), but higher doses elicit rise in BP and tachycardia which is probably due to
ganglionic stimulation (through ganglionic muscarinic receptors).
 Applied to the eye, it penetrates cornea and promptly causes miosis, ciliary muscle contraction and fall in intraocular
tension lasting 4–8 hours.
Therapeutic uses:
 Glaucoma
→ open angle glaucoma: third-line drug
→ Narrow angle glaucoma: principle drug after giving mannitol and acetazolamide (dec. IOT)
→ Pilocarpine is used only in the eye as 0.5–4% drops.
 counteract mydriatics after they have been used for testing refraction
 prevent/break adhesions of iris with lens or cornea by alternating it with mydriatics.
 Sialagogue in conditions like xerostomia resulting from radiotherapy etc.
Side effects:
 An initial stinging sensation in the eye
 Painful spasm of accommodation are frequent side effects.
 Pulmonary edema

ATROPINE:
 It is the prototype parasympatholytic drug.
 It is natural occurring alkaloidal ester of tropic acid with tropine base.
 It is obtained from Atropa Belladonna
PK:
 rapidly absorbed from g.i.t.
 Applied to eyes they freely penetrate cornea.
 About 50% of atropine is metabolized in liver and rest is excreted unchanged in urine.
 It has a t½ of 3–4 hours.
EFFECTS:
 CNS
→ Atropine stimulates many medullary centers—vagal, respiratory, vasomotor.
→ It depresses vestibular excitation and has anti-motion sickness property.
→ Blocks the relative cholinergic overactivity in basal ganglia
 CVS
→ Tachycardia, Decreased P-R interval, decreased A-V conduction (M2 receptor)
→ I.M./S.C. injection causes transient bradycardia due to blockade of muscarinic auto-receptors on vagal nerve endings.
 EYE
→ mydriasis, abolition of light reflex and cycloplegia lasting 7–10 days.
→ Photophobia and blurring of light vision.
 SMOOTH MUSCLES
→ Relaxation (M3 blockade)
→ Stomach and intestine contractions are decreased
→ Bronchodialation occurs
→ Relaxant action on urinary bladderand ureter.
 GLANDS
→ Atropine markedly decreases sweat, salivary, tracheobronchial and lacrimal secretion (M 3 blockade)
→ Atropine decreases secretion of acid, pepsin, mucus in the stomach, volume of secretion.

Sensitivity of organs:
 can be graded as—
Saliva, sweat, bronchial secretion > eye, bronchial muscle, heart > smooth muscle of intestine, bladder > gastric glands, smooth muscle

USES:
 Mydriatic and cycloplegic
Diagnostic use
→ For testing error of refraction, both mydriasis and cycloplegia are needed.
→ being highly potent used in children below 5 years. (Atropine ointment (1%))
Therapeutic use
→ Treatment of iritis, iridocyclitis, keratitis, corneal ulcer as it also has local anodyne effect.

 CARDIAC VAGOLYTIC:
→ Atropine is useful in counteracting sinus bradycardia and partial heart block in selected patients. (Digitalis toxicity)

 ANTIDOTE
→ Atropine is the specific antidote for anti-ChE(OP) and early mushroom poisoning.
→ In cobra bite along with neostigmine to prevent resp. paralysis

 PREANESTHETIC MEDICATION
→ Atropine is given along with GA(halothane) to prevent ventricular arrhythmias and also to prevent laryngeal spasm.

 Side effects:
→ Dry mouth,
→ Difficulty in swallowing and talking.
Dry, flushed and hot skin
→ difficulty in micturition
→ Decreased bowel sounds.
→ Dilated pupil, photophobia, blurring of near vision,
Excitement, psychotic behaviour, ataxia, delirium, dreadful visual hallucinations.
Hypotension, weak and rapid pulse, cardiovascular collapse with respiratory depression.
 Contra-indications
 Narrow angle glaucoma