Unit 2-ANS, Anticoagulants, Hemoglobin, Antimalarials, Histamine Flashcards
Common side effects of cholinomimetics
SLUDGE:
- Salivation
- Lacrimation
- Urination
- Diaphoresis
- GI Upset (diarrhea)
- Emesis (vomiting)
Bethanecol
Drug Class
Direct acting carbamic acid ester
(cholinomimetic)
Bethanecol
Mechanism
Direct-acting muscarinic cholinomimetic
Bethanecol
Uses
- Post-operative and neurogenic ileus;
- urinary retention (bowel and bladder smooth muscle ACh-innervated)
Bethanecol
Side effects
SLUDGE
Muscarine
Drug Class
Direct acting non-ester alkaloid
(cholinomimetic)
Muscarine
Mechanism
Direct-acting muscarinic cholinomimetic
Muscarine
Side Effects
SLUDGE
Pilocarpine
Drug Class
Direct acting non-ester alkaloid
(cholinomimetic)
Pilocarpine
Mechanism
Direct-acting muscarinic cholinomimetic
Pilocarpine
Uses
Glaucoma (ACh activates sphincter and ciliary muscles of eye)
Pilocarpine
Side effects
SLUDGE
Cevimeline
Drug Class
Direct acting non-ester alkaloid
(cholinomimetic)
Cevimeline
Mechanism
Direct-acting muscarinic cholinomimetic
Cevimeline
Uses
Dry mouth (in, e.g., Sjogren’s, post-radiation therapy; via increased salivation)
Cevimeline
Side effects
SLUDGE
Nicotine
Drug class
Direct acting non-ester alkaloid
(cholinomimetic)
Nicotine
Mechanism
Direct-acting nicotinic cholinomimetic
Nicotine
Uses
Smoking cessation (reduces cravings)
Neostigmine
Drug class
Indirect acting carbamate
(cholinomimetic)
Neostigmine
Mechanism
AChE inhibitor (short acting)
Lasts 0.5-2 hours
Neostigmine
Uses
- Post-operative and neurogenic ileus;
- urinary retention;
- myasthenia gravis;
- reversal of neuromuscular blockade
Neostigmine
Side effects
- SLUDGE + general increase in cholinergic neurotransmission;
- paralysis
Physostigmine
Drug class
Indirect acting carbamate
(cholinomimetic)
Physostigmine
Mechanism
AChE inhibitor (short acting)
Lasts 0.5-2 hours
Physostigmine
Uses
Glaucoma (ACh activates papillary sphincter and ciliary muscles of eye)
Physostigmine
Side effects
SLUDGE + general increase in cholinergic neurotransmission; paralysis
Donepezil
Drug Class
Indirect acting non-ester
(cholinomimetic)
Donepezil
Mechanism
AChE inhibitor
Donepezil
Uses
Alzheimer’s (amplifies endogenous ACh in brain)
Donepezil
Side effects
SLUDGE + general increase in cholinergic neurotransmission; paralysis
Edrophonium
Drug class
Indirect acting non-ester
(cholinomimetic)
Edrophonium
Mechanism
AChE inhibitor (v. short acting)
Lasts 5-15 minutes
Edrophonium
Uses
- Myasthenia gravis (differentiating deficiency versus ACh crisis);
- ileus
Edrophonium
Side effects
SLUDGE + general increase in cholinergic neurotransmission; paralysis
Ectothiophate
Drug Class
Indirect acting organophosphate
(cholinomimetic)
Ectothiophate
Mechanism
AChE inhibitor (long acting)
Lasts >100 hours
Ectothiophate
Uses
Glaucoma (ACh activates papillary sphincter and ciliary muscles of eye)
Ectothiophate
Side effects
SLUDGE + general increase in cholinergic neurotransmission; paralysis
Pralidoxime
Drug class
Strong nucleophile
(cholinomimetic)
Pralidoxime
Mechanism
Regenerates phosphorylated AChE
Pralidoxime
Uses
Poisoning by nerve gas, insecticide
Sarin
Drug class
Very potent indirect acting organophosphate
(cholinomimetic)
Sarin
Mechanism
AChE inhibitor
Sarin
Uses
Volatile nerve gas
Sarin
Side effects
- SLUDGE + general increase in cholinergic neurotransmission; paralysis
- Death
- Treat with pralidoxime and atropine before aging
Parathion
Drug class
Very potent indirect acting organophosphate
(cholinomimetic)
Parathion
Mechanism
AChE inhibitor
Parathion
Uses
Insecticide
Parathion
Side effects
- SLUDGE + general increase in cholinergic neurotransmission; paralysis
- Death
- Treat with pralidoxime and atropine before aging
Atropine
Drug Class
Tertiary amine antimuscarinic
(Cholinergic Receptor-Inhibitors)
Atropine
Mechanism
Blocks muscarinic receptors
Atropine
Uses
Mydriasis; cycloplegia
Atropine
Side effects
General block of muscarinic functions
Scopalamine
Drug class
Tertiary amine antimuscarinic
(Cholinergic Receptor-Inhibitors)
Scopalamine
Mechanism
Blocks muscarinic receptors
Scopalamine
Uses
Prevent or reduce motion sickness
Scopalamine
Side effects
General block of muscarinic functions
Dicyclomine
Drug class
Tertiary amine antimuscarinic
(Cholinergic Receptor-Inhibitors)
Dicyclomine
Mechanism
Blocks muscarinic receptors
Dicyclomine
Uses
Reduce transient hypermotility
Dicyclomine
Side effects
General block of muscarinic functions
Tropicamide
Drug class
Tertiary amine antimuscarinic
(Cholinergic Receptor-Inhibitors)
Tropicamide
Uses
Mydriasis; cycloplegia
Tropicamide
Side effects
General block of muscarinic functions
Tropicamide
Mechanism
Blocks muscarinic receptors
Very rapidly metabolized
Tolterodine
Drug class
Tertiary amine antimuscarinic
(Cholinergic Receptor-Inhibitors)
Tolterodine
Mechanism
Blocks muscarinic receptors
Tolterodine
Uses
Treat transient cystitis; postoperative bladder spasms; incontinence
Tolterodine
Side effects
General block of muscarinic functions
Benztropine
Drug Class
Tertiary amine antimuscarinic
(Cholinergic Receptor-Inhibitors)
Benztropine
Mechanism
Blocks muscarinic receptors
*crosses BBB*
Benztropine
Uses
Treat manifestations of Parkinson’s disease
Benztropine
Side effects
General block of muscarinic functions
Glycopyrrolate
Drug class
Quaternary amine antimuscarinic
(Cholinergic Receptor-Inhibitors)
Glycopyrrolate
Mechanism
Blocks muscarinic receptors
Glycopyrrolate
Uses
Reduce transient hypermotility
Glycopyrrolate
Side effects
General block of muscarinic functions
Tertiary vs Quaternary amine antimuscarinics
Tertiary: uncharged, crosses BBB
Quaternary: +charged; does not cross BBB
Ipatroprium
Drug class
Quarternary amine antimuscarinic
(Cholinergic Receptor-Inhibitors)
Ipatroprium
Mechanism
Blocks muscarinic receptors
Ipatroprium
Uses
Bronchodilation in asthma or COPD
Ipatroprium
Side effects
General block of muscarinic functions
Tiotroprium
Drug class
Quarternary amine antimuscarinic
(Cholinergic Receptor-Inhibitors)
Tiotroprium
Mechanism
Blocks muscarinic receptors
Tiotroprium
Uses
Bronchodilation in asthma or COPD
(Longer acting than ipratropium)
Tiotroprium
Side effects
General block of muscarinic functions
Hexamethonium
Drug Class
Ganglionic blocker
(Cholinergic Receptor-Inhibitors)
Hexamethonium
Mechanism
Blocks ganglionic (Nn) receptor and sympathetic tone
Hexamethonium
Uses
Hypertensive crisis; “Bloodless” field surgery
(rarely used now)
Mecamylamine
Drug Class
Ganglionic blocker
(Cholinergic Receptor-Inhibitors)
Mecamylamine
Mechanism
Blocks ganglionic (Nn) receptor and sympathetic tone
Mecamylamine
Uses
Hypertensive crisis; “Bloodless” field surgery
(rarely used now)
Succinylcholine
Drug class
Depolarizing blocker
(Cholinergic Receptor-Inhibitors)
Succinylcholine
Mechanism
Overstimulation of nicotinic receptor, leading to desensitization of muscle unit to further ACh stimulation
Succinylcholine
Uses
- Brief procedures (e.g., tracheal intubation, reset dislocated joints)
- Produces flaccid paralysis within 1 minute
Succinylcholine
Side effects
- Respiratory paralysis;
- disturbance of autonomic function
Tubocurarine
Drug class
Nondepolarizing blocker
(Cholinergic Receptor-Inhibitors)
Tubocurarine
Mechanism
- Blocks nicotinic (Nm) receptor
- Lasts 30-60 minutes
Tubocurarine
Uses
Muscle relaxant for surgery w/o deep anesthesia
Tubocurarine
Side effects
Respiratory paralysis; disturbance of autonomic function
Mivacurium
Drug Class
Nondepolarizing blocker
(Cholinergic Receptor-Inhibitors)
Mivacurium
Mechanism
- Blocks nicotinic (Nm) receptor
- Rapidly hydrolyzed, short acting
Mivacurium
Uses
Muscle relaxant for surgery w/o deep anesthesia
Mivacurium
Side effects
Respiratory paralysis; disturbance of autonomic function
Botulinum toxin
Drug class
Local paralytic
(Cholinergic Receptor-Inhibitors)
Botulinum toxin
Mechanism
Blocks vesicle fusion and ACh release on presynaptic terminal by degrading SNAP-25
Botulinum toxin
Uses
Reduce frown lines and wrinkles; achalasia; strabismus; oromandibular dystonia
Norepinephrine
Drug class
Non-selective agonist
(Adrenergic receptor agonist)
Norepinephrine
Mechanism
Agonist: α1, α2, β1
Norepinephrine
Uses
Acute Hypotension
Norepinephrine
Side effects
Hypertension; arrythmias; headache
Epinephrine
Drug class
Non-selective agonist
(adrenergic receptor agonist)
Epinephrine
Mechanism
Agonist: α1, (α2), β1, β2
Epinephrine
Uses
- Anaphylactic shock;
- combined with local anesthetics;
- glaucoma
Epinephrine
Side effects
Palpitation; arrhythmias; headache
Amphetamine
Drug class
Indirect acting
(Adrenergic receptor agonist)
Amphetamine
Mechanism
Increases release of NE
Amphetamine
Uses
ADHD, narcolepsy, recreation
Amphetamine
Side effects
Hypertension, insomnia, anxiety, arrhythmias
Isoproterenol
Drug class
Non-selective β agonist
(adrenergic receptor agonist)
Isoproterenol
Mechanism
Agonist: β1, β2
Isoproterenol
Uses
shock; heart block
Isoproterenol
Side effects
Palpitation; tachyarrhythmia; headache
Dobutamine
Drug class
β1-selective β agonist
(adrenergic receptor agonist)
Dobutamine
Mechanism
Agonist: β1
Dobutamine
Uses
Cardiac decompensation; shock; heart block
Dobutamine
Side effects
Tachyarrythmias; hypertension
Albuterol
Drug class
β2-selective β agonist
(adrenergic receptor agonist)
Albuterol
Mechanism
- Agonist: β2
- 10-15 minutes to take action, 6-12 hours (max) of duration; nebulizer delivers more, but greater side effects; oral is least effective (requires more dose –> side effects); can be used night symptoms, but not ideal
Albuterol
Uses
Prevent or reverse exercise-induced bronchospasm; mild asthma; COPD
Albuterol
Side effects
- Can mask progressively severe inflammation
- Tachycardia, muscle tremor
Terbutaline
Drug class
β2-selective β agonist
(adrenergic receptor agonist)
Terbutaline
mechanism
- Agonist: β2
- 10-15 minutes to take action, 6-12 hours (max) of duration; nebulizer delivers more, but greater side effects; oral is least effective (requires more dose –> side effects); can be used night symptoms, but not ideal
Terbutaline
Uses
- Prevent or reverse exercise-induced bronchospasm
- mild asthma
- COPD
- early labor
Terbutaline
Side effects
- Can mask progressively severe inflammation
- Tachycardia, muscle tremor
Phenylephrine
Drug Class
α1-selective α agonist
(adrenergic receptor agonist)
Phenylephrine
Mechanism
Agonist: α1
Phenylephrine
Uses
Nasal congestion; postural Hypotension
Phenylephrine
Side effects
Hypertension; reflex bradycardia
Clonidine
Drug class
α2-selective α agonist
(cholinergic receptor agonist)
Clonidine
Uses
Hypertension; shock; withdrawal from drug dependence
Clonidine
Side effects
Sedation
α-methyldopa
Drug class
α2-selective α agonist
(cholinergic receptor agonist)
α-methyldopa
Mechanism
Metabolite (a-methylnorepinephrine) activates CNS a2 receptors
α-methyldopa
Uses
Hypertension
α-methyldopa
Side effects
Sedation
Fenoldopam
Drug class
Selective dopamine agonist
Fenoldopam
Mechanism
Agonist: D1 only
~10 minute half-life
Fenoldopam
Uses
Increase blood flow at renal, mesenteric, and cerebral arteries
Dopamine
Drug class
Mixed acting (direct/indirect)
Dopamine
Mechanism
Agonist: D1, α1, β1
Low dose = Direct @ D1 Receptors
Medium dose = Direct @ Beta 1, some Indirect
High dose = Direct @ Alpha 1, some Indirect
Dopamine
Uses
Shock, renal failure, hypotension
Dopamine
Side effects
Vasoconstriction (@ high doses)
Phentolamine
Drug class
Non-selective α-antagonist
(adrenergic receptor antagonist)
Phentolamine
Mechanism
Antagonist: α1, α2
Phentolamine
Uses
Pheochromocytoma, Raynaud’s, frostbite
Phentolamine
Side effects
Postural hypotension; inhibit ejaculation
Phenoxybenzamine
Drug class
Non-selective α-antagonist
(cholinergic receptor antagonist)
Phenoxybenzamine
Mechanism
Antagonist: α1, α2; non-competitive blocker (covalent bond to receptor)
Phenoxybenzamine
Uses
Pheochromocytoma, Raynaud’s, frostbite
Phenoxybenzamine
Side effects
Postural hypotension; inhibit ejaculation
Prazosin
Drug class
α1-selective antagonist
(adrenergic receptor antagonist)
Prazosin
Mechanism
Antagonist: α1
Prazosin
Uses
Primary HTN, BPH
Prazosin
Side effects
Postural hypotension (usually 1st dose)
Terazosin
Drug Class
α1-selective antagonist
(cholinergic receptor antagonist)
Terazosin
Mechanism
Antagonist: α1
Terazosin
Uses
Primary HTN, BPH
Terazosin
Side effects
Postural hypotension (usually 1st dose)
Propranolol
Drug Class
Non-selective β-antagonist (1st generation)
Propranolol
Mechanism
Antagonist: β1, β2
Propranolol
Uses
Angina, Hypertension, Arrythmias
Propranolol
Side effects
Bradycardia, Bronchoconstriction, Sexual Dysfunction
Timolol
Drug class
Non-selective β-antagonist (1st generation)
Timolol
Mechanism
Antagonist: β1, β2
Timolol
Uses
Glaucoma
Timolol
Side effects
Bradycardia, Bronchoconstriction, Sexual Dysfunction
Metoprolol
Drug Class
β1-selective antagonist (2nd generation)
Metoprolol
Mechanism
Antagonist: β1
Metoprolol
Uses
HTN, Angina, Arrythmias, CHF
Metoprolol
Side effects
Bradycardia, Sexual Dysfunction
Atenolol
Drug Class
β1-selective antagonist (2nd generation)
Atenolol
Mechanism
Antagonist: β1
Atenolol
Uses
HTN, Angina, Arrythmias, CHF
Atenolol
Side effects
Bradycardia, Sexual Dysfunction
Bisoprolol
Drug class
β1-selective antagonist (2nd generation)
Bisoprolol
Mechanism
Antagonist: β1
Bisoprolol
Uses
HTN, Angina, Arrythmias, CHF
Bisoprolol
Side effects
Bradycardia, Sexual Dysfunction
Carvedilol
Drug class
Non-selective β-antagonist (3rd generation “A”)
Carvedilol
Mechanism
Antagonist: β1, β2
Carvedilol
Uses
CHF, HTN
Carvedilol
Side effects
Bradycardia, Fatigue
Labetalol
Drug class
Non-selective β-antagonist (3rd generation “A”)
Labetalol
Mechanism
Antagonist: β1, β2
Labetalol
Uses
CHF, HTN