Cholinergic Stimulants (Parasympathomimetics).pptx

1. Mention three types of polymers used in preparation of sustained release tablets?
A. HPMC
B. Polyvenyl alcohol
C. polyethylene oxide
2. What are the objectives of Novel Drug Delivery System?
A. Keeping the drug in the therapeutic range
B. Maintaining drug levels overnight
C. Reducing side effects by reducing dose frequency
3. Which is the classes of drug will be an ideal candidate for prolonged-release dosage forms?
Drugs with high solubility and high permeability.
4. Define Delayed-release dosage forms?
These release the drug at a time later than immediately after administration.
5. Define release liner?
a protective liner that is removed and discharged immediately before the application of the patch to skin.
6. Define backing laminate?
a backing layer, used as support in Transdermal patches.
7. What is the release profile in osmotic pump drug delivery system?
Zero order 1. Mention three types of polymers used in preparation of sustained release tablets?
A. HPMC
B. Polyvenyl alcohol
C. polyethylene oxide
2. What are the objectives of Novel Drug Delivery System?
A. Keeping the drug in the therapeutic range
B. Maintaining drug levels overnight
C. Reducing side effects by reducing dose frequency
3. Which is the classes of drug will be an ideal candidate for prolonged-release dosage forms?
Drugs with high solubility and high permeability.
4. Define Delayed-release dosage forms?
These release the drug at a time later than immediately after administration.
5. Define release liner?
a protective liner that is removed and discharged immediately before the application of the patch to skin.
6. Define backing laminate?
a backing layer, used as support in Transdermal patches.
7. What is the release profile in osmotic pump drug delivery system?
Zero order1. Mention three types of polymers used in preparation of sustained release tablets?
A. HPMC
B. Polyvenyl alcohol
C. polyethylene oxide
2. What are the objectives of Novel Drug Delivery System?
A. Keeping the drug in the therapeutic range
B. Maintaining drug levels overnight
C. Reducing side effects by reducing dose frequency
3. Which is the classes of drug will be an ideal candidate for prolonged-release dosage forms?
Drugs with high solubility and high permeability.
4. Define Delayed-release dosage forms?
These release the drug at a time later than immediately after administration.
5. Define release liner?
a protective liner that is removed and discharged immediately before the application of the patch to skin.
6. Define backing laminate?
a backing layer, used as support in Transdermal patches.
7. What is the release profile in osmotic pump drug delivery system?
Zero order1. Mention three types of polymers used in preparation of sustained release tablets?
A. HPMC
B. Polyvenyl alcohol
C. polyethylene oxide
2. What are the objectives of Novel Drug Delivery System?
A. Keeping the drug in the therapeutic range
B. Maintaining drug levels overnight
C. Reducing side effects by reducing dose frequency

1. Dr. mohammad dammag Level one Cholinergic Stimulants (Parasympathomimetics)

2. Cholinergic Stimulants (Parasympathomimetics) Definition : these are drugs that Stimulate muscarinic receptors 1- Direct acting Choline esters (quaternary amine) examples: A.ch., methacholine , carbachol and bethanechol . Cholinomimetic alkaloid example : Pilocarpine (tertiary amine)

3. Cholinergic Stimulants (Parasympathomimetics) 2- Indirect acting (anti- cholinesterase) a) Reversible : - physostigmine (tertiary amine) - neostigmine , pyridostigmine , edrophonium (quaternary ) . b) irreversible : - (Di-isopropyl- fluro -phosphate= DFP), parathion, malathion , metrifonate , Ecothiopate

4. Muscarinic actions : Eye : miosis, contract ciliary muscle, accommodate eye for near vision, ↑ aqueous drainage, ↓ I.O.P., ↑ lacrimation, conjunctival congestion . Secretions : ↑ salivary, bronchial, gastric and swcat secretions . Bradycardia ↓ A.V. conduction, ↓ B.P (Reversed by Atropine). ↑ gut motility. Contract wall of urinary bladder, relax sphincter → micturition 6-Bronchoconstriction Nicotinic actions : Skeletal muscle twitches 2-Reversal of hypotensive effect by atropine .

5. A)Choline esters :- quaternary amine, ionized, lipid insoluble, can't pass to brain, distributed extracellular.   A.Ch. Methacholine Carbachol Bethanechol True cholinesterase   Hydrolyzed Hydrolyzed --- --- Pseudocholinesterase   Hydrolyzed   --- --- Muscarinic actions   +++ +++ +++ +++ Nicotinic actions   +++ - +++ - Oral absorption   Not Incomplete Complete Selectivity   Not C.V.S Eye – GIT. – urinary tract Administration I.V Oral or S.C Oral or S.C Uses Not use Treatment(ttt ) of PAT (partial atrial tachycardia) diagnosis of 1-paroxysmal pheochromocytoma 2-bronchial asthma Glaucoma, paralytic ileus and non-obstructive urine retention Contraindications Bronchial asthma – peptic ulcer - ↓ H.R., ↓ B.P., thyrotoxicosis and not given I.M or I.V Antidote Atropine

6. B) Cholinomimetic alkaloid Examples: Pilocarpine : plant origin, tertiary amine ( Absorbed orally ,passes BBB). Mechanism of Action Acts directly on muscarinic receptors. Selective on eye & secretions. Clinical Uses treatment of glaucoma to antagonize mydriatics after fundus examination alternatively with mydriatics to cut adhesions between iris and lens. Also to ↑ salivation & sweat (diaphoretic in fever) .

7. 2. Indirect acting (Anticholinesterases ) They increase Acetyl choline. so act on muscarinic & nicotinic receptors Reversible : A-Physostigmine : B- Neostigmine (prostigmine) :

8. A-Physostigmine : Natural, plant origin ,Passes Blood brain barrier Tertiary amine ,Short duration of action , more specific on Eye. Actions : Muscarinic . Nicotinic . C.N.S stimulation → Convulsions. Uses : Local : on eye in treatment of glaucoma, to antagonize mydriatics, to cut adhesions between iris and lens. Systemic : in atropine poisoning. I.V.

9. B-Neostigmine (prostigmine) : Synthetic. Do not Passes Blood brain barrier Quaternary amine ,Long duration of action, more specific on Gastro-intestinal, urinary bladder. Actions : Muscarinic. Nicotinic. Stimulate skeletal muscle (direct). Uses : Diagnosis &treatment of myasthenia gravis I.M . Antidote to curare I.V. Paralytic ileus, Paroxysmal A trial Tachycardia( P.A.T)., urine retention(S.C,I.M) and atropine poisoning

10. • Pyridostigmine &ambenonium are used in treatment of myasthenia gravis. • Demecarium eye drops produces miosis, used in glaucoma. Edrophonium is Synthetic quaternary amine with 2-5 min duration due to rapid renal excretion. It is given I.V. Uses : diagnosis of myasthenia gravis to differentiate between cholinergic and myasthenic weakness(crisis). Also can be used in treatment of PAT(partial atrial tachycardia) antidote to curare.

11. New drugs in treatment of Alzheimer's Diseases Tacrine has anticholine esterase activity, used in Alzheimer's disease. Donepezil, Galantamine and rivastigmine are more selective cholinesterase inhibitor given one/day in Alzheimer's disease and are not hepatotoxic.

12. 2 - Irreversible (Organophosphorus compounds) They are non-competitive cholinesterase inhibitor Most of them are highly lipid soluble and can be absorbed from skin. Ecothiophate is lipid insoluble . Uses :- Insecticides : parathion, malathion , war gases : sarin , tabun , soman . Eye ointment in glaucoma: Isoflurophate Eye drops in glaucoma: Ecothiophate 203 weeks (long use → cataract). In bilharziasis (hematobium) : Metrifonate orally

13. Manifestations of Organophosphorus poisoning : Muscarinic: miosis, ↑ secretions, bronchospasm, ↓ H.R and B.P., vomiting, colic, diarrhea. Nicotinic: depolarization block inducing skeletal muscle paralysis. 3-C.N.S. stimulation (insomnia, convulsions) then coma. Death due to respiratory failure

14. Treatment of poisoning : Atropine I.V. or I.M. to antagonize muscarinic effects central & peripheral. Cholinesterase reactivators as pralidoxime , (PAM) , diacetylmonoxime (DAM) I.V. as early as possible. N.B.: Pralidoxime (PAM) cannot pass to C.N.S. but diacetylmonoxime (DAM) crosses blood brain barrier. 3.Care of respiration. 4.Anticonvulsants as diazepam. 5.Gastric lavage (if oral) & skin wash (if through skin).

15. Thank you