AKASH SYED(FA09-PHM-035)

Parasympathominetic

Direct Acting
Choline Esters
Classification:

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 (M3IP3+DAG---Gq) 2. Heart: (M2---Decrease CAMP---Gi) Decrease heart Rate 3. Blood Vessels: (M3---EDRF) Vasodilation. 4. Lungs: Brochocontractions (M3)
Pharmacodynamics:

AKASH SYED(FA09-PHM-035) Increase Brachial secretions. 5. GIT: Increase peristalsis (M3)

Increase secretionsSphincter relax 6. Urinary Bladder: Detrusor muscle contract Sphincter relax 7. Glands: Increase Lacrimal Increase Salivary (M3)

Therapeutic Uses:

1. Glaucoma: Increase drainage of aqueous humor 2. Post-operative atony. 3. Neurogenic Bladder: A lesion in the nervous tissue. 4. Myasthenia gravis: Autoimmune disease (Antibodies produce against Nm in body)

Adverse Effect:

1. Hypotension. 2. Diarrhoea 3. Enhanced secretions. 4. Bronchoconstriction. 5. Increase urinations.

Alkaloids
Classifications:

1. Nicotine

2. Lobeline 3. Pulocarpine 4. Muscarine

AKASH SYED(FA09-PHM-035)
Pharmacokinetics;

1. Tertiary Ammonium: (Nicotine, Lobeline, Pilocarpine ) these cant cross the CNS Directly. Can Cross GIT. 2. Quaternary Ammonium: (Muscarine) These can cross CNS. Cant cross GIT.

Pharmacodynamics:

1. Eye:

Miosis (Pilocarpine is a drug of choice in glaucoma. 2. Heart: Increase Rate (Cigarette having nicotine)

3. GIT: Increase peristalsis 4. Urinary System: Increase Voiding of urine. 5. Neuromuscular effect: Contraclity improves at low dose & muscle become flaccid at large dose.

Adverse Effect:

1. Hypertension. 2. Depolarizing blockade. 3. Tremers. 4. Nausea. 5. Vomiting. 6. Diarrhoea. 7. Increase Urination.

Indirect Acting
Classifications:
Reversible

AKASH SYED(FA09-PHM-035) 1. Edrophonium 2. Neostigmine. 3. Physostigmine. Irreversible 4. Parathion 5. Ecothiophate 6. Paraoxon 7. Malaoxon

Ist Step

2nd Step

Edrophonium Weak electrostatic bonds & hydrogen bonds. Its effect is 2 to 10min The effect of neostigmine and physostigmine is 30min-6hr. because these are carbonate esters. Irreversible inhibitors form colvent bond. 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.

Pharmacodynamics:
All of the cholinesters.

Therapeutic uses:
1. Glaucoma

AKASH SYED(FA09-PHM-035) 2. Myasthenia gravis 3. Atropine overdose.

Parasympatholytics
Antimuscrinics
Classifications:
1. Atropine. 2. Hyocine 3. Benztropine 4. Dicyclomine 5. Ipratropium 6. Pironzipine

Pharmacodynamics:
1. Eye: Mydriasis (Due to blocking of M3) Cyclopiegia in overdose.(Loss of accomondation for near visible, change of angle) Decrease lacrimal secretions. 2. Heart: Increase heart rate & contraction. 3. Respirtory System: Cause Bronchodilation. 4. GIT: Decrease peristalsis. 5. CNS: Drowsiness

Therapeutic Uses:
1. Parkinsonism Disease. (Benztropine)

AKASH SYED(FA09-PHM-035) 2. Motion sickness. (Scopolamine) 3. Travellers Diarrhoea. 4. Ophthalmologic examinations. 5. COPD. (Ipratropium). 6. Pre-anaesthetic medication . (becoz it reduces secretions & it effective against laryngospasm) 7. Urinary urgency due to inflammation of bladder. 8. Cholinergic poisoning.

Adverse effect:
1. Constipation. 2. Cycloplegia 3. Sandy eyes 4. Urinary retention. 5. Drowsiness

Ganglion Blocking Drugs

Classifications:
1. Tetraethyl ammonium (TEA) 2. Hexamethonium 3. Decamethonium 4. Mecamylamine 5. Trimethaphon

Pharmacokinetics:
TEA is not use as a drug becoz it has very short acting. First drug uses is hexamethonium for the treatment of hypertension.

Pharmacodynamics:
1. Eye: Mydriasis 2. Heart: Decrease Heart Rate

AKASH SYED(FA09-PHM-035) Decrease contractility 3. Blood vessels: Vasodilation. 4. CNS: No effect 5. GIT: Decrease peristalsis , decrease contractility.

Sympathomimetic
Classifications: DIRECT ACTING:
Selective alpha 1 agonist:
Phenylephrine Methoxamine Midodrine Oxymetazoline

It act on alpha2 also but less effect.

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. Eye: Mydriasis

MOA: alpha1 agonist ---Gq---IP3+DAG

(through relaxation of radial muscle).

2. Blood Vessels: Vasoconstriction. 3. Sphincters: Constriction of sphincters.

Clinical Uses:
1. Ophthalmological examination (facilitates the examination of retina). 2. Hypotension (cox it low BP).

AKASH SYED(FA09-PHM-035) 3. Nasal decongestant (due to vasoconstriction). 4. Use for reducing diffusion from the local anaesthetic.

Adverse effect:
Hypertension

Selective alpha2 agonist:

MOA: alpha2 selective agonist----decrease CAMP---Gi Organ system effect:
1. GIT(walls): decrease peristalsis (due to decrease release of acetylcholine from parasymthetic system).

Clinical Uses:
1. Glaucoma (Apraclonidine): cox it decease intraocular pressure & direct neuroprotective effect.

Mixed alpha, beta agonist:

Organ system effect: 1. Eye: Mydriasis 2. GIT: decrease pertislsis 3. Heart: increase heart rate 4. Respiratory System: Brochdilution 5. G