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Direct Acting
Choline Esters

1. Acetylcholine 2. Mathacholine 3. Carbachol 4. Bethanachol

Acetylcholine is not use as drug becoz its half-life is 5-20sec. Mathacholine is more resistant to hydrolysis & Carbonic acid esters are more resistant to hydrolysis by cholinesterase & therefore longer duration of actions. (Organ System Effect) 1. Eye: Miosis (M3—IP3+DAG---Gq) 2. Heart: (M2---Decrease CAMP---Gi) Decrease heart Rate 3. Blood Vessels: (M3---EDRF) Vasodilation. 4. Lungs: Brochocontractions (M3)

Bronchoconstriction. Pulocarpine 4. 5. Enhanced secretions. Glands: Increase Lacrimal Increase Salivary (M3) Therapeutic Uses: 1. Increase urinations. 4.AKASH SYED(FA09-PHM-035) Increase Brachial secretions. Urinary Bladder: Detrusor muscle contract Sphincter relax 7. 3. Post-operative atony. Nicotine 2. Neurogenic Bladder: A lesion in the nervous tissue. Muscarine . Diarrhoea 3. Lobeline 3. Hypotension. 5. GIT: Increase peristalsis (M3) Increase secretions…………Sphincter relax 6. Alkaloids Classifications: 1. 4. Glaucoma: Increase drainage of aqueous humor 2. Myasthenia gravis: Autoimmune disease (Antibodies produce against Nm in body) Adverse Effect: 1. 2.

Hypertension. Vomiting. Diarrhoea. Quaternary Ammonium: (Muscarine) These can cross CNS.AKASH SYED(FA09-PHM-035) Pharmacokinetics. Lobeline. 2. 5. Pilocarpine ) these cant cross the CNS Directly. Indirect Acting Classifications: Reversible . 2. 7. Can Cross GIT. Heart: Increase Rate (Cigarette having nicotine) 3. Increase Urination. Nausea. 6. Neuromuscular effect: Contraclity improves at low dose & muscle become flaccid at large dose. Cant cross GIT. 3. Depolarizing blockade. Eye: Miosis (Pilocarpine is a drug of choice in glaucoma. 2. 4. Pharmacodynamics: 1. Adverse Effect: 1. 1. 5. Urinary System: Increase Voiding of urine. Tertiary Ammonium: (Nicotine. GIT: Increase peristalsis 4. Tremers.

3. Glaucoma .AKASH SYED(FA09-PHM-035) 1. because these are carbonate esters. Paraoxon 7. Ecothiophate 6. Parathion 5. Aging: Aging is a process which involve further strengthening of enzyme-inhibitor bond & onces aging is occurred than pralidoxime(Cholinesterase regenerator) cant split the enzyme inhibitor bong. Irreversible 4. Edrophonium 2. Neostigmine. Irreversible inhibitors form colvent bond. Pharmacodynamics: All of the cholinesters. Therapeutic uses: 1. Physostigmine. It’s effect is 2 to 10min The effect of neostigmine and physostigmine is 30min-6hr. Malaoxon Ist Step 2nd Step Edrophonium Weak electrostatic bonds & hydrogen bonds.

Eye: Mydriasis (Due to blocking of M3) Cyclopiegia in overdose. Myasthenia gravis 3. 3. 2. Atropine. Dicyclomine 5. Ipratropium 6. Parkinsonism Disease. Heart: Increase heart rate & contraction. Pironzipine Pharmacodynamics: 1. 4. Benztropine 4. CNS: Drowsiness Therapeutic Uses: 1. GIT: Decrease peristalsis. Parasympatholytics Antimuscrinics Classifications: 1. 2.(Loss of accomondation for near visible. Respirtory System: Cause Bronchodilation. (Benztropine) . Atropine overdose.AKASH SYED(FA09-PHM-035) 2. change of angle) Decrease lacrimal secretions. 5. Hyocine 3.

Pre-anaesthetic medication . Eye: Mydriasis 2. First drug uses is hexamethonium for the treatment of hypertension. Constipation. Trimethaphon Pharmacokinetics: TEA is not use as a drug becoz it has very short acting. Ophthalmologic examinations. Decamethonium 4. Cycloplegia 3. Adverse effect: 1. Hexamethonium 3. Motion sickness. 5.AKASH SYED(FA09-PHM-035) 2. (becoz it reduces secretions & it effective against laryngospasm) 7. Cholinergic poisoning. 5. 8. Sandy eyes 4. Drowsiness Ganglion Blocking Drugs Classifications: 1. (Ipratropium). Heart: Decrease Heart Rate . Urinary urgency due to inflammation of bladder. Pharmacodynamics: 1. 4. 2. 6. COPD. Mecamylamine 5. (Scopolamine) 3. Tetraethyl ammonium (TEA) 2. Urinary retention. Traveller’s Diarrhoea.

AKASH SYED(FA09-PHM-035) Decrease contractility 3. GIT: Decrease peristalsis . Blood vessels: Vasodilation. CNS: No effect 5. decrease contractility. 4. . Sympathomimetic Classifications: DIRECT ACTING: Selective alpha 1 agonist: • • • • Phenylephrine Methoxamine Midodrine Oxymetazoline It act on alpha2 also but less effect.

Eye: Mydriasis MOA: alpha1 agonist ---Gq---IP3+DAG (through relaxation of radial muscle). Blood Vessels: Vasoconstriction. . 2. Clinical Uses: 1. 2. Sphincters: Constriction of sphincters. Hypotension (cox it low BP). Ophthalmological examination (facilitates the examination of retina). 3.AKASH SYED(FA09-PHM-035) Selective alpha 2 agonist: • • • • • • • • • • • Clonidine Methylnorepiephrine Norepinephrine (alpha 1 =alpha 2)(beta 1 >>beta 2) Epinephrine (alpha 1 = alpha 2)(beta 1 = beta 2) Dobutamine (beta 1> B2>>>>>alpha) Iso-prenaline (isoproterenol) (beta 1= beta 2) Salbutamol Terbutaline Albuterol Dopamine (D1=D2>>>beta>>>alpha ) (Non-selective) Fenoldoporm (D1>>D2) Mixed alpha beta agonist: Selective beta 2 agonist: Non-selective beta agonist: Selective beta 2 agonist: Dopamine Agonists: INDIRECT ACTING: • • • • Amphetamine Tyramine Pamoline Methylphenidate Selective alpha1 agonists: Organ system effect: 1.

4. G . Use for reducing diffusion from the local anaesthetic. Eye: Mydriasis 2. GIT(walls): decrease peristalsis (due to decrease release of acetylcholine from parasymthetic system). Adverse effect: Hypertension Selective alpha2 agonist: MOA: alpha2 selective agonist----decrease CAMP---Gi Organ system effect: 1. Heart: increase heart rate 4.AKASH SYED(FA09-PHM-035) 3. Glaucoma (Apraclonidine): cox it decease intraocular pressure & direct neuroprotective effect. GIT: decrease pertislsis 3. Nasal decongestant (due to vasoconstriction). Clinical Uses: 1. beta agonist: Organ system effect: 1. Respiratory System: Brochdilution 5. Mixed alpha.