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55 Cards in this Set

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Methacholine
ACh analogue, slowly hydrolysed by AChE
Carbachol
Analogue of ACh, resistant to AChE Used to treat glaucoma
Bethanechol
Analogue of ACh, resistant to AChE. Used to treat postop urinary retention, postop paralystic ileus, Xerostomia
Pilocarpine
Naturally occuring cholinomimetic alkyloid, from Pilocarpus jaborandi. Used to treat Glaucoma, Xerostima, and produce miosis
Muscarine
Naturally occuring cholinomimetic alkyloid, from Amantia muscarina.
Arecholine
Naturally occuring cholinomimetic alkyloid, from Betel nuts.
Atropine
Naturally occuring competitive reversible muscarinic receptor antagonist from Atropa belladonna. Blocks PSN. Used as antidote to block PSN stim, to produce mydriasis for eye examination or cosmetic. Emergency treatment of AChE inhibitor toxicity, emergency severe brachycardia, emergency asthma attacks when not responsive to B adrenergic agonists, peptic ulcers
Tetanus toxin
Cleaves synaptobrevin, preventing vesicle fusion. Used to relax muscles, reduce pain and severe underarm swelling.
Botulinum toxins B,D,F,G
Cleaves synaptobrevin, preventing vesicle fusion. Used to relax muscles, reduce pain and severe underarm swelling.
Botulinum toxins A,E
Cleaves SNAP-25, preventing vesicle fusion. Used to relax muscles, reduce pain and severe underarm swelling.
Botulinum toxin C1
Cleaves SNAP-25 and syntaxin, preventing vesicle fusion and ACh release. Used to relax muscles, reduce pain and severe underarm swelling.
Alpha-latrotoxin
Black widow spider poison, explosively stimulates Ca2+ dependent ACh release
Physostigmine
From the calabar bean. Reversible AChE inhibitor. Reduce amount of ACh hydrolysed at NMJ and some direct actication. Tertiary amine, therefore CNS signs. Moderatly lipid soluble. Causes miosis, antagonises atropine and curare. Used to treat glaucoma, could be used for myasthenia gravis
Neostigmine
Reversible AChE inhibitor. Reduce amount of ACh hydrolysed at NMJ and some direct actication. Quaternary amine, poor lipid solubility. More selective action at nicotinic muscular receptors than MRs. Restore strength in myasthenia gravis patients. Used to treat paralyic ileus and and urinary bladder atony.
Edrophonium
Reversible AChE inhibitor. Quaternary amine, very short acting, doesn't form covalent bond with AChE. Used in diagnosis of myesthenia gravis. Also used to establis doses of other AChE inhibitors
Isoflurophate (DFP)
Irreversible AChE inhibitor. Prototypical organophosphate. Lipid soluble, enters CNS.
Malathion
Irreversible AChE inhibitor. Used as an insecticide, must be metabolised to become active.
Parathion
Irreversible AChE inhibitor. Used as an insecticide, must be metabolised to become active.
Sarin gas
Irreversible AChE inhibitor. Used as a nerve gas. Volatile
Pralidoxime
Antidote to irreversible AChE inhibitor. Splits phosphodiester bond. Not well absorbed from GI tract, does not penetrate CNS - to be used in conjunction with atropine
Scopolamine
Muscarinic receptor antagonist. Tertiary amine. Found in Hycoscymas niger (henbane). Similar actions to atropine, but actions on CNS more important. Used to prevent motion sickness, preanaesthetic meds when parasympathomimetics involved, eye exams, peptic ulcers, Parkinson's
Nicotine
Ganglionic stimulant at autonomic ganglia, nicotinic receptors causing depolarisation. Larger doses, depolarisation is followed by depolarisation blockade. Stimulation followed by depression, stimulain of mesolimbic reward pressure, increased heart rate and blood pressure.
Hexamethonium
Ganglion blocking agent, blocks nicotinic receptors at autonomic ganglia. Effecs dependent on target organ
Mecamylamine
Ganglion blocker, only one still available today
Curare
Non depolarising, competitive blacker at NMJ, prevents ACh from binding. Paralyses white fibres more than red. Does not prevent release of ACh, can be competed away. diminished epps. not absorbed through GI tract, not cross BBB. Not metabolised, excreted by kidney. Used to relax muscles under anaesthesia
Atracurium
Compared to curare, faster onset, shorter duration and fewer side effects. Eliminated via spontaneous hydrolysis and plasma cholinesterases. Used to relax muscles under anaesthesia
Succinylcholine
Depolarising blocking agent. Interacts with nicotinic receptors at NMJ causing transient burts of APs, followed by inactivation. Short duration, hydrolysed by plasma cholinesterases. Used to relax muscles under anaesthesia
Alpha-methyltyrosine
Inhibits tyrosine hydroxylase -- blocks synthesis of NA.
Treatment of phenochromacytomas that make too much NA
Carbidopa
Inhibits DOPA carboxylase. Used to treat Parkinson's along with L-dopa to reduce peripheral side effects
Methyldopa
Metabolised into alpha-methylnoradrenaline - false transmitter. Stored and released in vesicles.
alpha1 less vasoconstriction
a2 presynaptic, greater effect inhibits neurotransmitter realease.
Antihypertensive.
Disulfiram
Inhibits dopamine beta hydroxylase and causes a partial depletion of NA stores
Reserpine
Alkaloid from Rauwolfia shrub. Binds tightly to catecholamine recognition site on storage vesicles. Blocks accumualtion of catecholamines by synaptic vesicles and therefore depletion by MAO. Used as an antihypertensive, but causes depression.
Tricyclic depressants (imipramine)
Cocaine
Inhibit uptake 1. Accumulation of NA at receptors and enhance sympathetic nerve activity. Also in CNS inhibit 5-HT uptake
Phenoxylbenzamine
Inhibit uptake 1
Alpha antagonist
-used for treating phaechromacytomas to block hypertensive effects
Entacapone
COMT inhibitor. Used to treat Parkinson's.
Clorgyline
MAO-A inhibitor.
Used to treat depression
Selegine
MAO-B inhibitor
Used to treat Parkinson's - potentiates remaining dopamine in substantia nigra.
Tranylcypromine
Iproniazid
Nonspecific inhibitors of MAO, increases cytoplasmic concentration of catecholamines so more leak out into the nerve terminal
Amphetamine
Tyramine
Ephedrine
Indirectly acting sympathomimetic agents. Uptake 1 then displace NA from vesicles. Have postsynaptic effects;
Ephedrine used as nasal decongestant, relieves bronchospasm by B2 effect
Guanethidine
Uptake 1, competes with NA. potentiates effects of exogenous catecholamines. Some NA leaks out and causes postynaptic stimulation intially. At low chronic doses, depletes NA stores and blocks neurones. In large doses causes inhibition of exocytosis. Was used as antihypertensives (also Bretylium)
Isoprenaline
Aderinergic beta1&2-agonist.
Was used to treat asthma as reduces bronchospasm.
Side effects tachycardia
Salbutamol
Aderinergic beta2-agonist.
Used to treat asthma (aerosol)
and premature uterine contractions
Dobutamine
Aderinergic beta1-agonist.
Given iv to give postitive ionotropic effect during cardiac shock. Also some use as heart block
Noradrenaline
Aderinergic beta1&alpha1-agonist.
IV pressor to raise blood pressure in shock or blood loss to allow perfusion of vital organs. No B2 effects, therefore better presser than Adr, even though lower A1 effects.
Adrenaline
Mixed aderinergic agonist.
Used in emergency situations:
-cardiac stimulant
-bronchodilator
-anaphylaxis(reverse vasodilation and bronchoconstriction)
Phenylephidrine
Aderinergic alpha1-agonist.
-local use for nasal congestion (vasoconstriction)
-causes hypertension and reflex brachycardia
Clonidine
Aderinergic alpha2-partial agonist.
-antihypertensive, lowers central sympathetic outflow
-introduce gradually and withdraw slowly
-help to treat opiate withdrawal
Yohimbine
Alpha adrenergic antagonist
not used therapeutically
Prazosin
Alpha adrenergic antagonist
Causes vasodilatation and relaxation of muscles in bladder neck (urinary retention)
Phentolamine
Alpha adrenergic antagonist. Some use in Raynaud's syndrome and peripheral vascular disease. Also to treat phaenochromocytoma
Propranalol
Beta adrenergic antagonist. Was used to treat hypertension, but side effects e.g. bronchoconstriciton
Atenolol
Practolol
Beta-1 adrenergic antagonists. Reduces effect of exercise on heart rate and arterial pressure
Caffeine
A1 receptor antagonist
increases wakefulness in CNS areas. Most prominent after prolonged wakefulness
Sildenafil
Inhibitor of type 5 phosphodiesterase. Stops degradation od cGMP to maintain contraction in smooth muscle cell. Viagra
L-NMMA (N MonoMethyl Arginine)
L-NAME (Nitro Arginine Methyl Ester)
L-NOARG (NitrO ARGine)
Inhibit NOS, analogues of L-arginine
D form inactive