Parasympathetic Flashcards by حكيم بورقيص

Selective Muscarinic 1 R blocker

Pirenzepine

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Selective M2 blocker

Gallamine

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Choline esters:

Ach, methacholine, carbachol, bethanechol

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Cholinomimetic alkaloids e.g

Pilocarpine

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Indirect-acting drugs (anticholinesterases:

Reversible: neostigmine and physostigmine
Irreversible: organophosphates
(Sarine, somain parathione and malathione)

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Ach

Quaternary ammonium
Must be given parenterally.
Non selective (Has both M and N action)
Not use clinically
Short duration

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What are the specific modifications in cholinergic agonist

– the susceptibillity of the compounds to hydrolysis by cholinesterase
Alter the relative activity on muscarinic and nicotinic receptors
Obtain therapeutically useful drugs

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T or F
All chline esters are tertiary ammonium compounds

F
All are quaternary

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Methachloline uses

It is given parentrally s.c for treatment of :
Paroxysmal atrial tachycardia

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Carbachol uses

Non selective and potent so it given to eye locllay for glucoma
Almost No major side effects.

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Bethanechol uses

GI disorders (paralytic ileus) postoperative non-obstructive abdominal distension, gastric atony and retension and gastroparesis
UB: postpartum or postoperative non-obstructive urinary retention.
Route of A: orally

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Adverse effects of bethanechol:

Due to generalized cholinergic stimulation:
Sweating, salivation, -BP & flushing (dt VD), nausea, abdominal pain, diarrhea and bronchospasm

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Uses of pilocarpine:

Glucoma (sornger than carbachol because it is tertiary)
Hair growth
Atropine poisoning

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Adverse effects of pilocarpine:

CNS disturbances (enters the brain)
Profuse sweating and salivation.

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Contra I of muscarinic Agonists:

Brochial asthma
Peptic ulcer disease
Coronary A disease
Hypotension or marked bradycradia
GIT hyper-motility
Parkinsonism

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Reversible Anti-cholinesterase:

A.alchohol with quaternary ammonium group : Endrophonium
B.carbamate derivatives : neostigmine (quaternary) and physostigmine (tertiary).

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Uses of Edorphonium:

Diagnosis of myasthenia gravis
Antidote for curare and curare like-agents.
Treatment of supraventricular tachy-arrythmias (but CCB best)

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Uses of reversible antiChE

Glucoma : physostigmine (eye d)
In anesthesia: Neostigmine (iv)
In intestinal and bladder atony : physostigmine & neostigmine
In treatment of myasthenia gravis
In atropine poisoning

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Dif b/w neostigmine and physostigmine:

Quaternary—tertiary
Poorly absorbed—-lipid s well a
No BBB —–cross BBB
On S.M —– On M R, Gang &CNS

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short essay about myasthenia gravis

An autoimmune disease, Ab formation against Nm- receptors of motor end plate
Characterized by muscle weakness with ++ fatigability resulting from failure of neuromuscular transmission

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Treatment of myasthenia gravis:

Neostigmine (orally 2-4h)
Pyridostigmine (orally 3-6h)
Edrophonium for diagnosis
Removing ABs by plasma exchage
– ABs production by steroids or immunesuppressant

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Reversible AntiChE with selective CNS effects:

Used in Alzheimer’s disease:
1.Tacrine (it has beem replaced because of ita hepatotoxicity).
2.Donepezil.
3.Rivastigmine
4.Galantamine

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Irreversible AntiChE:

Organ phosphorous compound:
War gases: somain & sarine
Insecticides:malathione&parathio
Metrifonate:oralAnti-Schistosoma
Isoflurophate :eye iont. Glucoma
Echothiophate: eye drop in glucoma

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Toxic manifest effects of irreversible ChE:

3 main types :
1.muscarinic :Dumbles
Nicotinic : muscle twiches & fasciculation, ++ adrenal medulla activity, tachycardia, cramping of S.M and HTN.
CNS: anxiety, restlessness, confusion, coma and depression of respiratory & CVS center

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Cause of death in irreversible anti-ChE:

Respiratory failure (central & peripheral)

Managemant of acutre toxicity of Anti-ChE

Dermal decontamination & gastric lavage Artificial respiration & suctioning of secretion Supportive treatment Toxin specific measures

Drugs used to treatment Oragonphosphorous poisoning:

1.Atropine to antagonize the muscarinic adverse effects 2.ChE reactivator : oxime 3.Pralidoxime (PAM) : (also reactivator 》 dephosphorylates AchE in the periphery) or Diacetylmonoxime 4.anti-convulsants e.g Diazepam 5.Fresh blood transfusion

Short assay about Diisopropylfluorophosphate (DFP):

Highly lipid soluble (well absorbed across all membranes, including skin. Used topically for treatment of chronic open-angle glucoma

Diisopropylfluorophsophate (DFP) adverse effects:

Local irritation of eye & headache

DFP and Echothiophate:

Echothiphate highly polar (poorly absorbed from GIT & has negligible distribution into CNS) Used as an aqueous solution for treatment of glucoma. Has adverse effects like DFP but less

N.m blockers:

Vecuronium, tubocuarine and pancuronium

Antimuscarinic agents:

Atropin, ipratropium

Ganglion blockers:

Nicotine in high dose

T or F Antimuscarinic or cholinergic antagonists block sympathetic neurons that are cholinergic innervated

T or F Cholinergic antagonists can block nicotinic receptors:

F They dont block nicotinic receptors, thus producing little or no action on skeletal neuromuscular junctions or autonomic ganglia.

Selective M3 blocker:

H.H.S.D (Hexa-Hydro-Sila-Difenidol)

Atropine causes B.D and decrease bronchial secretion. What is the better drug for this action?

Ipratropium

Atropine at large dose decreases gastric motility (antispasmodic effect) What is the better drug?

Pirenzepine

Atropine used in enuresis but there are better drugs:

TCA amd alpha-adrenergic antagonists

Atropine effects on Medulla:

Stimulation of the respiratory center and cardioinhibitory center and inhibitiom of the vomiting center

Atropine effects on basal ganglia:

Anti-parkinsonism

Atropine has ant-parkinsonism effects on basal ganglia but the ........ is more specific.

Benztropine

Uses of atropine:

1.Specific antidote for parasympathomimetic toxicity (organophosphorus poisoning, it is life saving) 2.Pre-anesthetic medication(4) 3.Heart block due to B-Blockers or digitalis. 4.in cases of vasovagal syncope dt excess vagal stimulation. 5.mydiatic for 2 puposes P32 6.peptic ulcer 7.intestinal and renal colic 8.diarrhea 9.nocturnal enuresis 10.hyperhydrosis 11.Vomiting and motion sickness 12.parkinsonism

Atropine used in intestinal and renal colic but ........ is more specific and for vomiting but ........ is better

Hyoscine butyl bromide Hyscine

Atropine is used for nocturnal enuresis but ......... is better

Emepronium

Atropine adverse effects:

زغولة النشفة حبست جوزها بوسريع +cycloplegia Central excitation (irritability and hyperactivity)

Atropine toxicity:

Sever tachycardia and dilated pupil Toxic psychosis Respiratory depression may occu Fever dt dryness Abdominal distension dt paralysis of peristalsis Retention of urine Allergic manifestations.

Treatment of atropine toxicity:

1. I.V physostigmine for ++ Ach cenrally and peripherally (BBB) 2.Diazepam iv for convulsions 3.in severe cases :artificial repirati 4.Stomach wash if taken orally 5.Ice bags and cold fomentations

Explain why? Antipyretics are not effective in the case of atropine toxicity.

Because the sweating is inhibitrd.

Contraindications of atropine:

Fevers, Glucoma, bronchial Asthma, Tachycardia, Paralysis ileus, senile hypertrophy of prostate After neostigmine as it may lead to severe Bradycardia. Allergy to atropine

Hyoscine is similar to atropine but:

Has shorter duration Mainly depressant effect on CNS leading to sedation & amnesia More effective on eye Less on heart and GIT (no tachy) No local anodyne action on the skin or MM

Uses of hyoscine:

Pre-anesthetic medication Prophylaxis of motion sickness Parkinsonism & Meniere's disease

Hyoscine is better than atropine in pre-anesthetic dt:

C.N.S depression and amnesia (less anesthetic is needed) Stimulation of the R.C Strong anti-secretory effect (prevent aspiration pneumonia) No tachycardia, safe in thyrotoxic patients.

Atropine substitutes Mydriatic cycloplegic group:

Eye drops : Homatropine, tropicamide and cyclopentolate

Mydriatic but non cycloplegic atropine substitutes:

Eucatropine

Antisecretory & antispasmodic atropine substitutes:

Atropine methyl nitrate, hyoscine Butyle Bromide, oxphenonium, propantheline

Pirenzepine (gastrozepine) & telenzepine

Selective M1 blocker that inhibit gastric secretion It is useful in peptic ulcer

In theraputic doses,they have antimuscarinic effects specific on GIT In large doses ganglion blocking effects and neuromuscular blocking effects

Atropine methyl nitrate, hyoscine butyl bromide, oxphenonium, propantheline

Atropine substitutes specific on the urinary bladder:

Emepronium (cetriprin) & oxybutynin (uripan) Quaternary ammonium compound

Antiasthmatic Atropine substitute affects s.m of the bronchi but doesn't affect glands of the mucosa

Ipratropium

Antiparkinsonian Atropine substitutes:

Benzotropine (cogentin), trihexphendyle (artane)

Ganglion stimulant short assay:

1.Stimulate both symp and para 2.They are not in common use 3.in cause stim in low dose and vas versa 4

Ganglion stimulant their actions are similar to nicotine May given intra umblical in neonatal asphyxia:

Lobeline

Nicotinic effects(MTWHF)

Mydriasis, Tachycardia, weakness, hypertension, fasciculations

T or F Ganglion blockers are pure antagonists. They don't produce initial stimulation

Parasympathetic Flashcards

(65 cards)