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فارما > Parasympathetic > Flashcards

Parasympathetic Flashcards

1
Q

Selective Muscarinic 1 R blocker

A

Pirenzepine

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2
Q

Selective M2 blocker

A

Gallamine

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3
Q

Choline esters:

A

Ach, methacholine, carbachol, bethanechol

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4
Q

Cholinomimetic alkaloids e.g

A

Pilocarpine

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5
Q

Indirect-acting drugs (anticholinesterases:

A

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

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6
Q

Ach

A

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

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7
Q

What are the specific modifications in cholinergic agonist

A

– 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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8
Q

T or F
All chline esters are tertiary ammonium compounds

A

F
All are quaternary

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9
Q

Methachloline uses

A

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

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10
Q

Carbachol uses

A

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

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11
Q

Bethanechol uses

A

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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12
Q

Adverse effects of bethanechol:

A

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

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13
Q

Uses of pilocarpine:

A

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

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14
Q

Adverse effects of pilocarpine:

A

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

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15
Q

Contra I of muscarinic Agonists:

A

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

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16
Q

Reversible Anti-cholinesterase:

A

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

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17
Q

Uses of Edorphonium:

A

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

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18
Q

Uses of reversible antiChE

A

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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19
Q

Dif b/w neostigmine and physostigmine:

A

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

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20
Q

short essay about myasthenia gravis

A

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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21
Q

Treatment of myasthenia gravis:

A

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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22
Q

Reversible AntiChE with selective CNS effects:

A

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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23
Q

Irreversible AntiChE:

A

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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24
Q

Toxic manifest effects of irreversible ChE:

A

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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25
Q

Cause of death in irreversible anti-ChE:

A

Respiratory failure (central & peripheral)

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26
Q

Managemant of acutre toxicity of Anti-ChE

A

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

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27
Q

Drugs used to treatment Oragonphosphorous poisoning:

A

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

28
Q

Short assay about Diisopropylfluorophosphate (DFP):

A

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

29
Q

Diisopropylfluorophsophate (DFP) adverse effects:

A

Local irritation of eye & headache

30
Q

DFP and Echothiophate:

A

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

31
Q

N.m blockers:

A

Vecuronium, tubocuarine and pancuronium

32
Q

Antimuscarinic agents:

A

Atropin, ipratropium

33
Q

Ganglion blockers:

A

Nicotine in high dose

34
Q

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

A

T

35
Q

T or F
Cholinergic antagonists can block nicotinic receptors:

A

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

36
Q

Selective M3 blocker:

A

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

37
Q

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

A

Ipratropium

38
Q

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

A

Pirenzepine

39
Q

Atropine used in enuresis but there are better drugs:

A

TCA amd alpha-adrenergic antagonists

40
Q

Atropine effects on Medulla:

A

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

41
Q

Atropine effects on basal ganglia:

A

Anti-parkinsonism

42
Q

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

A

Benztropine

43
Q

Uses of atropine:

A

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

44
Q

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

A

Hyoscine butyl bromide
Hyscine

45
Q

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

A

Emepronium

46
Q

Atropine adverse effects:

A

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

47
Q

Atropine toxicity:

A

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.

48
Q

Treatment of atropine toxicity:

A
  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
49
Q

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

A

Because the sweating is inhibitrd.

50
Q

Contraindications of atropine:

A

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

51
Q

Hyoscine is similar to atropine but:

A

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

52
Q

Uses of hyoscine:

A

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

53
Q

Hyoscine is better than atropine in pre-anesthetic dt:

A

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.

54
Q

Atropine substitutes
Mydriatic cycloplegic group:

A

Eye drops :
Homatropine, tropicamide and cyclopentolate

55
Q

Mydriatic but non cycloplegic atropine substitutes:

A

Eucatropine

56
Q

Antisecretory & antispasmodic atropine substitutes:

A

Atropine methyl nitrate, hyoscine Butyle Bromide, oxphenonium, propantheline

57
Q

Pirenzepine (gastrozepine) & telenzepine

A

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

58
Q

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

A

Atropine methyl nitrate, hyoscine butyl bromide, oxphenonium, propantheline

59
Q

Atropine substitutes specific on the urinary bladder:

A

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

60
Q

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

A

Ipratropium

61
Q

Antiparkinsonian Atropine substitutes:

A

Benzotropine (cogentin), trihexphendyle (artane)

62
Q

Ganglion stimulant short assay:

A

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

63
Q

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

A

Lobeline

64
Q

Nicotinic effects(MTWHF)

A

Mydriasis, Tachycardia, weakness, hypertension, fasciculations

65
Q

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

A

T

فارما (10 decks)

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