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PHARMACOLOGY SEMMELWEIS > Cholinergic & Adnrenergic + NMJ, Anaesthetic > Flashcards

Cholinergic & Adnrenergic + NMJ, Anaesthetic Flashcards

Cholinergic & Adrenergic + NMJ, Anaesthetic

1
Q

Direct-acting cholinomimetics : 4 choline esters (only 1 in the list)

A

Acetylcholine, Methacholine, Carbachol(B3), Bethanechol

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2
Q

Direct-acting cholinomimetics : 3 alkaloids (only 1 in the list)

A

Muscarine, Nicotine, Pilocarpine(B3)

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3
Q

Direct-acting cholinomimetics : 1 synthetic (not in the list)

A

Varenicline(not in the list)

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4
Q

About Acetylcholine(not in the list)

A

M and N, short half life, only use in opthalmology

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5
Q

About Methacholine(not in the list)

A

Non-selective, Methacholine provocation test, Challenge test for diagnosis of asthma(differential diagnosis of bronchial hyperactivity)

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6
Q

About Bethanechol(not in the list)

A

M, Oral, 30min-2hr, resistant to AChe, Non-obstructive ileus, Urinary retention

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7
Q

About Carbachol(B3)

A

M and N, Topical, resistant to AChe, Constricts pupil and relieves intraocular pressure in open-angle glaucoma

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8
Q

About Muscarine(not in the list)

A

M, Quatenary amine, Mushroom posion

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9
Q

About Nicotine(not in the list)

A

N, tertiary amine, plant-derived poison

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10
Q

About Pilocarpine(B3)

A

M, Oral, tertiary amine, 30-2hr, Glaucoma(eye drop), Xerostomia(sjogren syndrome)

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11
Q

About Varenicline(not in the list)

A

N partial agonist, smoking cessation

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12
Q

Indirect-acting cholinomimetics : acetylcholinesterase inhibitors : 6 carbamates

A

Neostigmine(B3), Pyridostigmine(B3), Physostigmine, Rivastigmine(B3), Galantamine(not in the list), Donepezil (not in the list)

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13
Q

Indirect-acting cholinomimetics : acetylcholinesterase inhibitors : 3 organophosphates (not in the list)

A

Malathion, Parathion, Sarin

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14
Q

Indirect-acting cholinomimetics : acetylcholinesterase inhibitors : 1 Alcohol

A

Edrophonium(B3)

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15
Q

AchE inhibitors poisoning (Muscarinic effects)

A

DUMBBELS D: Diarrhea U: Urination M: Miosis B: Bradycardia B: Bronchoconstriction E: Excitation(CNS, muscles) L: Lacrimation S: Secretion

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16
Q

About Neostigmine

A

Quaternary amine, 2-4 h, Myasthenia gravis, Non-obstructive ileus, Urinary retention

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17
Q

About Pyridostigmine

A

Quaternary amine, 3-6h, Myasthenia gravis

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18
Q

About Physostigmine

A

Tertiary amine, 0.5 2h, Antidote in atropine overdose (iv), Glaucoma treatment(topical)

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19
Q

About Rivastigmine, Galantamine, Donepezil

A

Tertiary amine, half life 70hr, Alzheimer disease(transdermal patch)

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20
Q

About Malathion, Parathion(not in the list)

A

Drug activation via P450 reaction (Malaoxon, Paraoxon) Insecticide

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21
Q

About Sarin(not in the list)

A

Rapid action, Nerve gas(lethal)

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22
Q

About Edrophonium(B3)

A

half life (5-10min), no CNS effect Diagnosis of Myasthenia gravis(improved muscle tone->positive diagnosis) Differential diagnosis (Tensilon test) : cholinergic crisis vs Myasthenia crisis

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23
Q

Indirect-acting cholinomimetics : acetylcholinesterase inhibitors : Competitive 2 drugs (only one in the list)

A

Edrophonium (B3), doenepezil (not in the list)

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24
Q

Indirect-acting cholinomimetics : acetylcholinesterase inhibitors : non competitive 4 drugs (1 not in the list)

A

Physostigmine (not in the list), Rivastigmine(B3), Neostigmine(B3), Pyridostigmine(B3)

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25
Q

Cholinoceptor blockers-cholinergic antagonists : 10 muscarinic antagonists (1 not in the list)

A

Atropine(B4), Cyclopentolate(B4), Scopolamine(B4), Butyl-scopolamine(B4), Procyclidine(B4, A34), Benztropine(not in the list), Solifenacin(B4), Oxybutynin(B4), Ipratropium(B4), Tiotropium(B4)

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26
Q

About Atropine(B4)

A

Non-selective, Alkaloid, Plant-derived, Tertiary amine, 2–4 h action Mydriatic and cycloplegic agent - ophthalmology Antispasmodic, antisecretory, antidiarrheal Reverasal of AV block Management of Bradyarrhthmia (iv) Antidote for Cholinesterase inhibitor toxicity

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27
Q

About Cytclopentolate(B4)

A

Non-selective, Mydriatic and cycloplegic agent (eyedrop)

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28
Q

About Scopolamine(B4)

A

Non-selective, Tertiary amine, Motion sickness (transdermal patch)

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29
Q

About Butyl-scopolamine(B4)

A

Non-selective, no CNS effects used to treat pain and discomfort caused by abdominal cramps, menstrual cramps, or other spasmodic activity in the digestive system

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30
Q

About Procyclidine(B4, A34), Benztropine(not in the list)

A

Non-selective, Tertiary amine, Oral, Parenteral Parkinson disease

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31
Q

About Solifenacin(B4), Oxybutynin(B4)

A

Modest selectivity for M3, Oral, Transdermal patch Urinary incontinence

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32
Q

About Ipratropium(B4)

A

Non-selective, inhaled, Bronchodilator for asthma/COPD - Side effects: dry mouth, cough

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33
Q

About Tiotropium(B4)

A

M3-selective, longer duration, inhaled Bronchodilator for asthma/COPD - Side effects: dry mouth, cough

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34
Q

Cholinoceptor blockers-cholinergic antagonists : 3 tertiary tropeins (2 in the list)

A

Atropine(B4), Scopolamine(B4), Benztropine (not in the list)

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35
Q

Cholinoceptor blockers-cholinergic antagonists : 4 synthetic drugs with tertiary amine

A

Procyclidin(A34, B4), Cyclopentolate(B4), Solifenacine(A35), Oxybutynin(A35)

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36
Q

Cholinoceptor blockers-cholinergic antagonists : 3 Quaternary tropeins

A

Butyl-scopolamine(A35, B4), Ipratropium(B4), Tiotropium (B4)

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37
Q

Adverse effects- Muscarinic antagonists

A
  • Decreased secretions (salivary, bronchiolar, sweat) - Mydriasis, cycloplegia → blurred vision - Hyperthermia (with resulting vasodilation) - Tachycardia - CNS effects (sedation, hallucination) - Urinary retention - Constipation
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38
Q

Cholinesterase regenerators (not in the list)

A

Pralidoxime(2-PAM) Chemical antagonist of organophosphate Antidote for organophosphate poisoning

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39
Q

3 Drugs for pre-synaptic inhibition (one in the list)

A

Hemicholinium : Inhibits transport of choline into the nerve terminal Vesamicol : Inhibits transport of Ach into storage vesicles Botulinum toxin(B9) : Inhibits release of Ach-loaded vesicles (interfere with SNARE proteins), Blepharospasm, hyper-hydrosis, dystonia, Cosmetics

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40
Q

Botulinum toxin(B9)

A

Direct-acting muscle relaxants - Prevents synaptic exocytosis through inhibition of SNARE fusion proteins in presynaptic nerve terminals → flaccid paralysis - Direct injection into muscle - Duration of action 2-3 months - Upper and lower limb spasm due to cerebral palsy, multiple sclerosis - Cervical dystonia - Migraine - Overactive bladder - Hyperhidrosis - Cosmetics

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41
Q

2 Drugs for pre-synaptic stimulation (not in the list)

A

4-aminopyridine : K+-channel blocker → membrane depolarization → Ca2+ influx → release of Ach alpha-Latrotoxin : Creates pores along membrane → Ca2+ influx → release of Ach (Spider venom)

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42
Q

5 Direct-acting sympathomimetics (catecholamines)

A

Epinephrine, Norepinephrine, Dopamine, Isoprenaline (Isoproterenol), Dobutamine

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43
Q

About Epinephrine (B5)

A

α1, α2, β1, β2 Pharmacologically: - Parenteral administration only (no oral) - Short duration of action - No CNS entry Dose-dependent effects: - Low-dose: β1, β2 stimulation predominates (HR, SV, CO, pulse pressure ↑, TPR, BP ↓, bronchodilation) - High-dose: α1 stimulation predominates (TPR, BP ↑, reflex bradycardia) Pharmacological indications: - Cardiac arrest, complete heart block - Anaphylactic (distributive) shock - Hypotensive emergency - Adjunct to local anesthetics (reduce local blood flow) - Acute asthma attack Side effects: hypertension, arrhythmia, stroke, myocardial infarction, pulmonary edema

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44
Q

About Norepinephrine (B5)

A

α1, α2, β1 Pharmacologically: - Parenteral administration only (no oral) - Short duration of action - No CNS entry - Cardiac arrest, complete heart block - Hypotensive emergency - Adjunct to local anesthetics (reduce local blood flow) - Shock (cardiogenic, neurogenic, septic) Side effects: vasospasm, tissue necrosis, hypertension, arrhythmia, infarction

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45
Q

About Dopamine (B5)

A

D1, α1, α2, β1, β2 Pharmacologically: - Parenteral administration only (no oral) - Short duration of action - No CNS entry Dose-dependent effects: - Low-dose: D1 stimulation (renal perfusion↑) - Medium dose: β1 stimulation (cardiac stimulation) - High-dose: acts like epinephrine (loses selectivity) Pharmacological indications: - Shock (especially with renal failure) Side effects: arrhythmia

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46
Q

About Isoprenaline (Isoproterenol) (B5)

A

β1 = β2 - Parenteral administration - Cardiac arrest, complete heart block (IV) - Acute asthma attack (nebulizer)

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47
Q

About Dobutamine

A

β1 > β2 >>> (α1) - Parenteral administration - Cardiogenic shock - Acute heart failure - Cardiac stimulation in cardiac stress-test

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48
Q

7 α-agonists (non-catecholamines)

A

Phenylephrine, Oxymetazoline, Clonidine, Rilmenidine, Methyldopa, Brimonidine, Tizanidine

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49
Q

About Phenylephrine (B6)

A

α1-agonist - Not inactivated by COMT – longer duration of action compared to catecholamines - Oral, parenteral - Duration of action 15-60 min’ - Ophthalmologic use (mydriatic agent) - Decongestant - Hypotension treatment (TPR↑, mean BP↑) Side effects: reflex bradycardia, hypertension, stroke, MI, ischemic changes of mucus membrane

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50
Q

About Oxymetazoline (B6)

A

Local α1-agonist Systemic α2-agonist - Topical - Decongestant Side effects: hypotension due to α2 clonidine-like effect

51
Q

About Clonidine (B6)

A

α2-agonist I2-agonist - Imidazole derivative → agonist for both imidazole receptor (I2) and α2 receptors - Oral or transdermal patch - Antihypertensive (pre-synaptic sympatholytic effect) - Attention-deficit hyperactivity disorders (ADHD) - Tourette’s syndrome - Alcohol/opiates withdrawal syndrome Side effects: sedation, dry mouth, severe rebound hypertension if suddenly stopped, drug-induced lupus

52
Q

Rilmenidine (B6)

A

α2-agonist, I2-agonist -Imidazole derivative → agonist for both imidazole receptor (I2) and α2 receptors - Antihypertensive (pre-synaptic sympatholytic effect) Side effects: milder compared to clonidine

53
Q

Methyldopa (B6)

A

α2-agonist, I2-agonist - Imidazole derivative → agonist for both imidazole receptor (I2) and α2 receptors - Antihypertensive (pre-synaptic sympatholytic effect) Side effects: sedation, drug-induced lupus

54
Q

Brimonidine (not in the list)

A

α2-agonist - Topical (eye drops) - Glaucoma (aqueous humour production ↓)

55
Q

Tizanidine (B9)

A

α2-agonist - Oral - Centrally-acting muscle relaxant

56
Q

4 Release-inducing agents Displace stored catecholamines from nerve endings

A

Amphetamine, Methylphenidate, Tyramine, Ephedrine

57
Q

Amphetamine (not in the list)

A
  • Enter CNS - Resistant to metabolism by MAO - long duration of action - Attention-deficit hyperactivity disorders (ADHD) - Central nervous system disorders (narcolepsy) - Psychostimulant due to central release of DA, NE, 5-HT - Appetite suppression - Drug of abuse (high addiction liability) Side effects: seizures, aggression, insomnia, hypertension
58
Q

Methylphenidate (not in the list)

A
  • Amphetamine derivative - Attention-deficit hyperactivity disorders (ADHD) - Narcolepsy
59
Q

Tyramine (not in the list)

A
  • Oral bioavailability is limited due to rapid metabolism by MAO-A in gut and liver - MAO-A inhibition results in increased bioavailability, potential hypertensive crisis (“cheese effect”) - No clinical use - Found in fermented foods (red wine, cheese) - Psychoactive peripheral sympathomimetic effects
60
Q

Ephedrine (B6)

A
  • Plant-derived alkaloid - Oral bioavailability ↑, duration of action ↑ - Direct and indirect sympathomimetic effects - Stimulant, appetite suppressant, concentration aid - Decongestant - Treatment of hypotension associated with anaesthesia - Lower addiction liability than amphetamines
61
Q

3 Reuptake inhibitors Increase the activity of neurotransmitters in the synapse by inhibiting their reuptake into the pre-synaptic nerve terminal

A

Cocaine, Atomoxetine, Modafinil

62
Q

Cocaine (A5)

A
  • Enter CNS - Inhibits both NET and DAT - Drug of abuse - Local anesthetic + vasoconstrictor Side effects: hypertension, coronary spasm, chest pain, acute MI, arrhythmias, seizures
63
Q

Atomoxetine(not in the list)

A
  • Selective NE reuptake inhibitor - Attention-deficit hyperactivity disorders (ADHD)
64
Q

Modafinil (not in the list)

A
  • Inhibits both NET and DAT - Improve wakefulness in narcolepsy and other conditions
65
Q

3 MAO inhibitors Inhibit the metabolism of catecholamines by monoamine oxidase enzyme (MAO)

A

Tranylcypromine, Moclobemide, Selegiline

66
Q

Tranylcypromine (not in the list)

A

Non-selective - Irreversible inhibitor - Antidepressant (no longer in clinical use)

67
Q

Moclobemide (A29)

A

MAO-A selective - Reversible inhibitor - Antidepressant

68
Q

Selegiline (A34)

A

MAO-B selective - Reversible inhibitor - Parkinson disease

69
Q

Direct-acting sympatholytics – α adrenoreceptor antagonists : 2 Non-selective α-receptor antagonists (only 1 in the list)

A

Phentolamine(B7), Phenoxybenzamine (not in the list)

70
Q

Phentolamine(B7)

A

non-selective - Reversible inhibition - Duration of action 2-4 h’ orally, 20-40 min’ parenterally - Pre-operative management of pheochromocytoma - Antidote in case of acute hypertension due to α-agonist overdose (cocaine, amphetamine, tyramine) Side effects: orthostatic hypotension with subsequent reflex tachycardia

71
Q

Phenoxybenzamine (not in the list)

A

α non-selective - Irreversible, non-competitive inhibition (covalent binding to the receptor) - Duration of action up to 48 h’ - Pre-operative management of pheochromocytoma - Antidote in case of acute hypertension due to α-agonist overdose (cocaine, amphetamine, tyramine) Side effects: orthostatic hypotension with subsequent reflex tachycardia

72
Q

Direct-acting sympatholytics – α adrenoreceptor antagonists : 5 Selective α-receptor antagonists (3 in the list)

A

Prazosin(B7), Doxazosin(B7), Tamsulosin(B7), Urapidil(not in the list), Mirtazapine(not in the list)

73
Q

Prazosin(B7)

A

α1-selective - Oral - Duration of action 8-24 h’ - Hypertension - Benign prostatic hyperplasia (BPH) → relax the muscle of the prostate and bladder neck, which allows urine to flow more easily Side effects: orthostatic hypotension (mainly in first doses)

74
Q

Prazosin(B7), Doxazosin(B7), Tamsulosin(B7)

A

α1-selective - Oral - Duration of action 8-24 h’ - Hypertension - Benign prostatic hyperplasia (BPH) → relax the muscle of the prostate and bladder neck, which allows urine to flow more easily Side effects: orthostatic hypotension (mainly in first doses)

75
Q

Urapidil(not in the list)

A

α1 antagonist α2 weak agonist 5-HT weak agonist β antagonist - Oral - Hypertension, hypertensive crisis - Benign prostatic hyperplasia (BPH)

76
Q

Mirtazapine(not in the list)

A

α2-selective - Oral - Antidepressant (inhibitory effect on pre-synaptic α2-receptors in CNS → increased release of NE and 5-HT)

77
Q

Direct-acting sympatholytics – β adrenoreceptor antagonists : 4 Non-selective β-receptor antagonists

A

Propranolol(B8), Timolol(B8), Pindolol(B8), Sotalol(B8, B16)

78
Q

Propranolol(B8)

A

β non-selective - Oral, parenteral - High lipid-solubility (freely enter CNS) - Duration 4-6 h’ - Local anesthetic effect (inhibit Na+ channels) - Angina (HR↓ → diastolic perfusion↑, O2 demand ↓) - Anti-arrhythmic class II (treatment and prophylaxis) - Hypertension - Thyrotoxicosis - Migraine (prophylaxis) - Essential tremor

79
Q

Pindolol(B8)

A

β non-selective - Intrinsic sympathomimetic activity (ISA) - Local anesthetic effect (inhibit Na+ channels) - Hypertensive treatment in asthmatic/COPD patients - Should be avoided in HF

80
Q

Timolol(B8)

A

β non-selective - Topical - Glaucoma (aqueous humor production ↓)

81
Q

Sotalol(B8, B16)

A

β non-selective K+-channel antagonist - Oral - Duration if action 7 h’ - Anti-arrhythmic class III (ventricular arrhythmias, AF) - Side effects: dose-dependent Torsade-de-Pointes

82
Q

Direct-acting sympatholytics – β adrenoreceptor antagonists : 5 Selective β-receptor antagonists (cardio-selective) (4 in the list)

A

Metoprolol(B8), Bisoprolol(B8), Nebivolol(B8), Esmolol(B8, B16), Acebutolol(Not in the list)

83
Q

Metoprolol(B8)

A

β1-selective - Duration 6-9 h’ - Local anesthetic effect (inhibit Na+ channels) - Hypertension - Congestive heart failure (reduce mortality) - Angina pectoris - Anti-arrhythmic - Acute coronary syndrome (ACS)

84
Q

Bisoprolol(B8)

A

β1-selective - Long duration of action (10-12 h’) - Hypertension - Congestive heart failure (reduce mortality) - Angina pectoris - Anti-arrhythmic - Acute coronary syndrome (ACS)

85
Q

Nebivolol(B8)

A

β1-selective - NO-dependent vasodilating action - Hypertension - Congestive heart failure (reduce mortality) - Angina pectoris - Anti-arrhythmic - Acute coronary syndrome (ACS)

86
Q

Esmolol(B8, B16)

A

β1-selective - IV - Short duration of action (∼10 min’) - Arrhythmias associated with thyroid-storm or perioperative (acute management) - Hypertensive emergencies

87
Q

Acebutolol (Not in the list)

A

β1-selective - Intrinsic sympathomimetic activity (ISA) - Hypertensive treatment in asthmatic/COPD patients

88
Q

Direct-acting sympatholytics – β adrenoreceptor antagonists : 2 Combined α and β receptors antagonists

A

Carvedilol(B7, B8), Labetalol (not in the list)

89
Q

Carvedilol(B7, B8)

A

β1 β2 antagonist α1-antagonist - Oral, IV - Duration of action 5 h’ - Congestive heart failure (reduce mortality) - Hypertension - Hypertensive emergencies (IV)

90
Q

Labetalol (not in the list)

A

β1 β2 antagonist α1-antagonist - Oral, IV - Duration of action 5 h’ - Congestive heart failure (reduce mortality) - Hypertension - Hypertensive emergencies (IV)

91
Q

2 Indirect-acting sympatholytic (not in the list)

A

Metyrosine, Reserpine

92
Q

Metyrosine(not in the list)

A
  • Competitive inhibitor of tyrosine hydroxylase enzyme (rate-limiting step in endogenous catecholamine synthesis) - Reduces synthesis of dopamine, norepinephrine, and epinephrine - Pheochromocytoma
93
Q

Reserpine(not in the list)

A

Inhibits uptake of norepinephrine into storage vesicles, resulting in depletion of catecholamines and serotonin from central and peripheral axon terminals - Antihypertensive - Antipsychotic - Huntington’s disease (adverse effects limit its clinical use)

94
Q

Local Anesthetics : 3 amides

A

Lidocain(A5, B16), Articaine(A5), Bupivacaine (A5)

95
Q

Lidocain(A5, B16)

A
  • Topical use or injection (perineural, epidural, subarachnoid); rarely used IV - Hepatic metabolism via CYP450 - Duration of action 1-2 h’, with epinephrine 2-4 h’ - Short-duration, local surgical procedures (dental, ophthalmology, throat, urology, obstetrics) - Post-operative analgesia - Produce autonomic blockade in ischemic conditions - Side effects: excitation, seizures, vasodilation, hypotension, arrhythmias *Risk of drug-induced methemoglobinemia
96
Q

Articaine(A5)

A
  • Onset of action is the most rapid of all local anesthetics - Short-duration, local surgical procedures (dental, ophthalmology, throat, urology, obstetrics) - Post-operative analgesia - Produce autonomic blockade in ischemic conditions - Side effects: excitation, seizures, vasodilation, hypotension, arrhythmias *Risk of drug-induced methemoglobinemia
97
Q

Bupivacaine (A5)

A
  • Parenteral (usually not topical or IV) - Hepatic metabolism via CYP450 - Duration of action 3-6 h’ - Longer-duration, local surgical procedures - Side effects: CNS toxicity, cardiovascular collapse
98
Q

Local Anesthetics : 3 Esters (1 in the list)

A

Procaine(not in the list), Tetracaine(not in the list), Cocaine(A5)

99
Q

Procaine(not in the list)

A
  • Parenteral (usually not topical or IV) - Metabolism by plasma cholinesterase (pseudocholinesterase) - Duration of action 30-60 min’, with epinephrine 60-90 min’ - Short-duration, local surgical procedures - Side effects: excitation, seizures, vasodilation, hypotension, arrhythmias
100
Q

Tetracaine(not in the list)

A
  • Duration of action 2-3 h’ - Used primarily for spinal anesthesia
101
Q

Cocaine(A5)

A
  • Intrinsic sympathomimetic effect due to its inhibition of norepinephrine reuptake into nerve terminals - Topical or parenteral - Metabolism by plasma cholinesterase (pseudocholinesterase) - Duration of action 1-2 h’ - Procedures requiring high surface activity and vasoconstriction - Drug of abuse - Side effects: CNS excitation (psychostimulant), convulsions, cardiac arrhythmias, hypertension, coronary vasospasm *except for cocaine, all local anesthetics are vasodilators
102
Q

About Neuromuscular blocking agents

A

Act locally, at the level of the neuromuscular junction, to produce muscle paralysis 1. Non-depolarizing agents Competitive antagonists at skeletal muscle Ach nicotinic receptors (NM); parenteral administration Indications: - Prolonged relaxation for surgical procedures - Relaxation of respiratory muscles to facilitate mechanical ventilation in ICU patients - Epileptic seizure (convulsion) not responding to antiepileptics - Intoxication with certain drugs (theophylline, amphetamine) 2. Depolarizing agents - Agonist at skeletal muscle Ach nicotinic receptors (NM); may stimulate ganglionic nicotinic Ach receptor (NN) and cardiac muscarinic Ach receptors (M3) - Phase I → membrane depolarizes, resulting in an initial discharge that produces transient contraction (fasciculations/twitch), followed by flaccid paralysis - Phase II → membrane repolarizes, but receptor is desensitized to the effect of Ach (succinylcholine is still bound to the receptor)

103
Q

Neuromuscular blocking agents : Non-depolarizing agents : 4 isoquinoline

A

D tubocurarine(B10), Atracurium(B10), Cisatracurium(B10), Mivacurium(B10)

104
Q

D tubocurarine(B10)

A

isoquinoline Intermediate-acting (25-45 min’) Renal mechanism - Histamine release (hypotension) - Prolonged apnea (muscle weakness)

105
Q

Atracurium(B10)

A

isoquinoline Intermediate-acting (25-45 min’) Spontaneous metabolism - Histamine release (hypotension) - Muscle spasm (muscle weakness)

106
Q

Cisatracurium(B10)

A

isoquinoline Intermediate-acting (25-45 min’) Spontaneous metabolism - Histamine release (hypotension) - Prolonged apnea (muscle weakness)

107
Q

Mivacurium(B10)

A

isoquinoline Short-acting (10-15 min’) Pseudocholinesterase (metabolism) - Histamine release (hypotension) - Prolonged apnea (muscle weakness)

108
Q

Neuromuscular blocking agents : Non-depolarizing agents: 4 steroids (2 in the list)

A

Pancuronium(B10), Rocuronium(not in the list), Vecuronium(not in the list), Pipecuronium(B10)

109
Q

Pancuronium(B10)

A

Long-acting (60-180 min’) Renal metabolism - M2-inhibition (tachycardia) - NE reuptake inhibition

110
Q

Rocuronium(not in the list)

A

Intermediate-acting (25-45 min’) Hepatic metabolism - Prolonged apnea (muscle weakness)

111
Q

Vecuronium(not in the list)

A

Intermediate-acting (25-45 min’) Hepatic metabolism - Prolonged apnea (muscle weakness)

112
Q

Pipecuronium(B10)

A

Long acting (60 180 minutes) renal metabolism

113
Q

Neuromuscular blocking agents : 1 depolarizing agents:

A

Succinylcholine(B10)

114
Q

Succinylcholine(B10) (suxamethonium)

A

-Selective agonist of the Nm receptor receptor and the acetylcholinesterase does not metabolize it - Parenteral - Duration of action 5 min’ - Rapid metabolism by pseudocholinesterase in the blood then in liver - Surgical procedures where a rapid onset and brief duration is needed (intubation, endoscopy, ECT) - Side effects: arrhythmias(mainly bradycardia), hyperkalemia, transient increased intra-abdominal and intraocular pressure, postoperative muscle pain, Malignant hyperthermia (highlighted in the lecture)

115
Q

About Spasmolytic agents

A

Act centrally, at the level of the CNS, to reduce abnormal muscle tone caused by neurologic/muscle end-plate disease (causing spasm and associated muscle pain). The goal is to reduce excessive skeletal muscle tone without reduction of strength; reduced muscle spasm results in reduction of pain and improved morbidity.

116
Q

4 Spasmolytic agents

A

Diazepam(A25, A33,B9), Baclopen(B9), Tizanidine(B9), Tolperisone(B9)

117
Q

Diazepam(A25, A33,B9)

A

GABAA agonist - Increases interneuron inhibition of primary motor afferents in spinal cord - Hepatic metabolism - Duration of action 12-24 h’ - Chronic spasm due to cerebral palsy, stroke, spinal cord injury - Acute spasm due to muscle injury - Side effects: CNS depressant actions, tolerance, dependent liability

118
Q

Baclopen(B9)

A

GABAB agonist - Pre- and postsynaptic inhibition of motor output in the spinal cord - Oral, intrathecal - Spasm due to cerebral palsy, multiple sclerosis, stroke - Side effects: sedation, weakness,

119
Q

Tizanidine(B9)

A

α2 agonist - Pre- and postsynaptic inhibition of reflex motor output in the spinal cord - Oral - Renal and hepatic elimination - Duration of action 3-6 h’ - Spasm due to multiple sclerosis, stroke, amyotrophic lateral sclerosis - Side effects: weakness, sedation, hypotension, hepatotoxicity (rare), rebound hypertension upon abrupt withdrawal

120
Q

Tolperisone(B9)

A
  • Poorly understood inhibition of muscle stretch reflex in spinal cord and brain stem → reduction of muscle reflexes - Mechanism involved inhibition of Na+ and Ca2+ channels - Oral - Acute spasm due to muscle injury - Not used in chronic spasm - Side effects: sedation, confusion, ocular effects, strong anti-muscarinic effect
121
Q

2 Direct-acting muscle relaxants

A

Dantrolene(9), Botulinum toxin(B9)

122
Q

Dantrolene(9)

A
  • RyR1 antagonist → Blocks Ca2+-release channels in the sarcoplasmic reticulum of skeletal muscle → reduces actin-myosin interaction - IV, oral - Duration of action 4-6 h’ - Malignant hyperthermia (IV) - Spasm due to cerebral palsy, spinal cord injury, multiple sclerosis (oral) - Side effects: muscle weakness, hepatotoxicity
123
Q

Botulinum toxin(B9)

A
  • Prevents synaptic exocytosis through inhibition of SNARE fusion proteins in presynaptic nerve terminals → flaccid paralysis - Direct injection into muscle - Duration of action 2-3 months - Upper and lower limb spasm due to cerebral palsy, multiple sclerosis - Cervical dystonia - Migraine - Overactive bladder - Hyperhidrosis - Cosmetics

PHARMACOLOGY SEMMELWEIS (54 decks)

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