Help
Options
Didn't know it?
click below
click below
Knew it?
click below
click below
Don't Know
Remaining cards (0)
Know
retry
shuffle
restart
0:00
Embed Code - If you would like this activity on your web page, copy the script below and paste it into your web page.
Normal Size Small Size show me how
Normal Size Small Size show me how
PDA II - Exam 2
MoA/Classes/random
| Question | Answer |
|---|---|
| hemicholinium | blocks active transport of choline |
| vesamicol | blocks active transport of ACh into vesicle |
| botulinum toxin | blocks proteins that are needed to cause vesicles to fuse & release ACh |
| acetylcholinesterase (AChE) | terminates actions of ACh through metabolism |
| catecholamines | NE, epi, dopamine |
| nicotinic receptors | excitatory; located at ganglia of SNS and PSNS; also skeletal muscle receptors on muscle |
| muscarinic receptors | metabotropic; located at the end organs of the PSNS |
| M 1, 3, 5 odd numbers | coupled to Gq which activates phospholipase C leading to 2nd messengers IP3 and DAG --> incr intracellular Ca++ levels effects: incr secretions from glands, incr contractions of GI, bladder, bronchial smooth muscle |
| M 2, 4 even numbers | coupled to Gi or Go which inhibits adenylate cyclase (cAMP formation), this inhibits voltage-gated channels, and activates K+ channels effect: slow HR and contraction |
| adrenergic receptors | alpha and beta |
| a 1 receptors | subdivided into 1A, 1B, 1D major func: vasoconstriction linked to Gq proteins and coupled to phospholipase C and A to produce 2nd messengers IP3, Dag, and archidonate |
| a 2 receptors | subdivided into 1A, 2B, 2C major func: acts on neurones to decrease further release of NT's!!! linked to Gi proteins (inhibitory proteins) and coupled to adenylate cyclase to inhibit cAMP |
| B receptors | all of these linked to Gs proteins which are coupled to adenylate cyclase to inhibit cAMP |
| B1 receptors | heart; major function is to act to increase HR and force of contraction |
| B2 receptors | blood vessels; major functino is to cause relaxation of smooth muscle - blood vessels, bronchioles, GI tract and eye |
| B3 receptors | major function may be in lipolysis and thermogenesis |
| a-methyltyrosine (Metyrosine) | adrenergic: inbhibits tyrosine hydroxylase; adrenergic; sometimes used to treat pheochromocytoma (tumor relasing too much epi and NE) |
| tyramine | adrenergic: a "false transmitter" which displaces NE found in foods such as cheese, wine, some meats |
| ephedrine | adrenergic: enhances release of NE and acts as an ALPHA and BETA agonist adverse effect can be HTN ma huang contains ephedrine |
| amphetamine | adrenergic: enhances release of NE and acts as an ALPHA and BETA agonist |
| reserpine | adrenergic: blocks the vesicular MA transporter depleting NE (won't store or transport) - first drug found to interfere with SNS, earliest antiHTN |
| dimethylphenylpiperazinium (DMPP) | nicotinic agonist stimulates autonomic ganglionic cells selectively |
| trimethaphan | ganglionic blocking agent (nicotonic antagonist) |
| hexamthonium | ganglionic blocking agent (nicotonic antagonist) |
| atropine | non-selective muscarinic antagonist TERTIARY amine - used to be given for eye exams? from Atropa Belladonna (Deadly Nightshade) more later |
| newer subtype selective cholinergic antagonist | pirenzepine (M1) |
| newer subtype selective cholinergic antagonist | tripitramine (M2) |
| newer subtype selective cholinergic antagonist | darifenacin (M3) |
| phenylephrine | A1 AGonist |
| clonidine | A2 AGonist |
| isoproterenol | B AGonist (non-selective) |
| dobutamine | B1 AGonist |
| terbutaline | B2 AGonist |
| prazosin | A1 ANTAGonist |
| yohimbine | A2 ANTAGonist |
| atenolol | B1 ANTAgonist |
| neostigmine | AChE inhibitor |
| cocaine | blocks NE transporter (reuptake) |
| selegiline | MAOI (MAO metabolizes catecholamines) |
| acetylcholine | DIRECT acting cholinergic agonist - choline ester acts at muscarinic and nictonic receptors NOT used clinically bc it's not selective and is susceptible to rapid hydrolysis QUATERNARY Nitrogen |
| methacholine | DIRECT acting cholinergic agonist - choline ester |
| carbachol | DIRECT acting cholinergic agonist - choline ester |
| bethanechol | DIRECT acting cholinergic agonist - choline ester |
| muscarine | DIRECT acting cholinergic agonist - naturally occurring alkaloid QUATERNARY Nitrogen |
| pilocarpine | DIRECT acting cholinergic agonist - naturally occurring alkaloid TERTIARY Nitrogen |
| arecoline | DIRECT acting cholinergic agonist - naturally occurring alkaloid |
| nicotine | DIRECT acting cholinergic agonist - naturally occurring alkaloid |
| methacholine (B-methylcholine acetate) | muscarinic agonist; NO activity at nicotinic receptors (because of the methyl group attached to the carbonyl/nicotinic side of the molecule) |
| Bethanecol (B-methylcholine carbamate) | LONG-acting SELECTIVE muscarinic agonist - carbamate slows hydrolysis and the beta methyl changes the selectivity to muscarinic |
| acetylcholinesterase inhibitors (AChEI) | INDIRECT acting cholinergic agonist compete with ACh for active site on AChE (ACh - parasympathomimetic (mimicking actions/helping actions of ACh) |
| pyridostigmine | non-competitive reversible ACh inhibitor - carbamic acid derivative TERTIARY amine |
| neostigmine | non-competitive reversible ACh inhibitor - carbamic acid derivative TERTIARY amine |
| physiostigmine | non-competitive reversible ACh inhibitor - carbamic acid derivative TERTIARY amine |
| demarcarium | non-competitive reversible ACh inhibitor - carbamic acid derivative |
| ambenonium | non-competitive reversible ACh inhibitor - carbamic acid derivative |
| echotiophate | irreversible inhibitor of ACh - organophosphate |
| parathion | irreversible inhibitor of ACh - organophosphate - insecticide |
| malathion | irreversible inhibitor of ACh - organophosphate - insecticide |
| organosphosphates | bind irreversibly to active site of ACh Esterase; causes the HoH step fo the reaction to be slower if not absent |
| 2-PAM (2-pyridineal doximethyliodide) | antidotal therapy for organophosphates - attracted to the anionic site (serine) on enzyme --> regenerate the enzyme AND generate an inactive poison molecule - has to be given IMMEDIATELY |
| pralidoxime | antidotal therapy for organophosphates - attracted to the anionic site (serine) on enzyme --> regenerate the enzyme AND generate an inactive poison molecule - has to be given IMMEDIATELY |
| organophosphates - nerve gasses | sarin, soman, tabun |
| AChE Function | nucelophilic attack by serine hydrolyzes ACh giving choline and an acetylated enzyme; acteylated enzyme is rapidly hydrolyzed to regenerate the active enzyme |
| reversible inhibiton of AChE | nucleophilic attack by serine hydrolyzes drug to give a carbamalated enzyme; carbamalated enzyme can't breakdown ACh; the carbamylated enzyme is slowly hydrolyzed and eventually the regerated enzyme is active again |
| irreversible inhibition of AChE | nucleophilic attach by serine hydrolyzes drug/toxin to give a phosphorylated enzyme; phosphorylated enzyme is VERY resistant to hydrolysis, especially after "aging" (2-PAM can dephosphorylate enzyme if aging hasn't occurred) |
| SLUDGE | cholinergic - parasympathomimetic salivation, lacrimation, urination, diarrhea, gastric emptying, emesis |
| DUMBELS | cholinergic - parasympathomimetic diarrhea/diaphoresis, urination, miosis, bradycardia/bronchorrhea, emesis/emptying, lacrimation, salivation |
| MTWHFS | cholinergic - nicotinic mydriasis, tachycardia, weakness, hypertension, fasciculations, seizures |
| carbachol (Isopto-carbachol) | DIRECT acting cholinergic agonist - tx for glaucoma |
| pilocarpine (Isopto-carpine, Ocusert) | DIRECT acting cholinergic agonist - tx for glaucoma |
| physostigmine (Isopto-eserine) | INDIRECT acting cholinergic agonist - tx for glaucoma |
| echotiophate (Phospholine iodide) | INDIRECT acting cholinergic agonist - tx for glaucoma |
| cholinergic agonists for glaucoma - mech of action | allow for increased drainage via canal and meshwork net effect: increase aqueous humor outflow, decrease IOP |
| cholinergic agonists for glaucoma - side effects | blurred far vision diminished visual acuity in low light both tend to diminish with chronic use |
| also useful in glaucoma | beta blocker - decrease inflow of fluid |
| clinical uses of cholinergic agonists | GI or GU disorders Myasthenia gravis (and Alzheimers?) - diagnostic test and tx prophylaxis in cholinesterase poisoning |
| bethanechol (Urecholine) | DIRECT acting cholinergic agonist - orally or SQ induces peristaltic activity of the gut and stimulates bladder contraction |
| bethanechol contraindications | peptic ulcers UT obstruction anything else PSNS - side effects |
| edrophonium | INDIRECT cholinergic agonist - blocks AChE diagnostic test for M gravis VERY SHORT ACTING |
| pyridostigmine (Mestinon) | INDIRECT cholinergic agonist - AChE inhibitor, REVERSIBLE oral admin, slow onset (1-2 hr), LONG duration of action (8-12 hr) - tx of M gravis |
| neostigmine (Prostigmine | INDIRECT cholinergic agonist - AChE inhbitor, REVERSIBLE oral admin, RAPID onset (10-30 min), intermediate duration of action (2-4 hr) - tx of M gravis |
| pyridostigmine | prophylaxis for cholinesterase poisoning? not used for this anymore though (because it penetrates the BB barrier and causes issues) |
| anticholinergic effects | anti-SLUDGE dry mouth dry eyes tachycardia urinary retention decr gastric scretion & GI motility (low dose effects listed first) |
| agonists | slim sleek basic, tend to be hydrophilic job = to activate receptor (full = efficacy) |
| antagonists | bulkly, hydrophilic job = to cover the receptor (full = no "efficacy") |
| ipratropium | anti-cholinergic QUATERNARY amine |
| tiotropium | anti-cholinergic QUATERNARY amine |
| scopolamine | anti-cholinergic TERTIARY amine |
| homatropine (Isopto homatropine) | anti-cholinergic - clinical use for eye exams TOPICAL admin, minimal systemic effects; duration of action 30-90 min |
| tropicamide (Mydriacil) | anti-cholinergic - clinical use for eye exams TOPICAL admin, minimal systemic effects; duration of action 30-90 min |
| cyclopentolate (Cyclogyl) | anti-cholinergic - clinical use for eye exams TOPICAL admin, minimal systemic effects; duration of action 30-90 min |
| anti-cholinergics for eye dilation | produce mydriatic (dilation) and cycloplegic (fixed far vision) effects reduction in lacrimal secretions no major effect on IOP SEs: photophobia, blurred near vision |
| anti-cholinergics for cardiovascular | increase HR (block vagus nerve) no major change in BV tone (no effect on BP even though CO increases) |
| atropine | anti-cholinergic cardiovascular use coronary care units/surgical wards - to stop vagal tone (incr) from decreasing heart rate SE = ATROPINE FLUSH (body can't sweat) |
| anti-cholinergics for respiratory SE's = dry mouth | blocks PSNS tone acting with SNS to control bronchodilation blocks PSNS invoked response to allergens and chemicals clinical uses = bronchodilation (effect more pronounced in COPD pts), during surgery |
| ipratropium (Atrovent) | anti-cholinergic for bronchodilation in asthma and COPD pts - good at preventing constriction not stopping it (bad rescue agent) |
| tiotropium (Spiriva) | anti-cholinergic for bronchodilation in asthma and COPD pts - good at preventing constriction not stopping it (bad rescue agent) |
| anti-cholinergics to prevent choking in surgery | including atropine... to prevent increased secretions of mouth and lungs due to drugs (anesthetics, morphine, NMJ blockers) from accumulating - will prevent these secretions! results in super dry mouth |
| anti-cholinergics gastro-intestinal effects | reduce salivary secretions reduce gastric acid secretion (although H2 blockers and PPIs more effective for PUD and GERD) relaxation of GI smooth muscle - clinically not used as much bc questionable efficacy and need high doses (more SE's) |
| dicyclomine (Bentyl) | has some anti-cholinergic actions used for cramping |
| anti-cholinergics genitourinary uses and SE's | uinhibited bladder syndrome, bladder spasms, OA bladder, incontinence, enuresis SE's: xerostomia, blurred vision, constipation (peripheral M3) drowsiness, DZ, confusion (more in elderly - central M1 effects) |
| oxybutynin (Ditropan) | genitourinary Anti-cholinergic high incidence of antimusc effects, particularly dry mouth TRANSDERMAL and TOPICAL admin better tolerated |
| tolterodine (Detrol) | genitourinary Anti-cholinergic seems to have selectivity for bladder tissue - better tolerated |
| tropsium (Sanctura) | genitourinary Anti-cholinergic QUATERNARY amine limits CNS effects |
| solifenacin (Vesicare) | genitourinary Anti-cholinergic suggested to be more selective for M3 receptor over M1 --> reduced CNS side effects |
| darifenicin (Enablex) | genitourinary Anti-cholinergic suggested to be more selective for M3 receptor over M1 --> reduced CNS side effects |
| physostigmine | NEVER USE IN A PT WITH EKG ABNORMALITY - can result in vagal block - normally tx for anticholinergic overdose |
| atropine overdose | CNS problems can get so bad that it can result in convulsions and death body temp goes WAY up |
| anti-cholinergics for cholinergic crisis/poisonings | - overdose of chol agonists or AChE inhibitors for MG or AD - organophosphate poisoning (2-PAM and atropine) |
| nicotine | ganglionic drug low dose - stimulatory on N receptors high - produces depolarizing blockade drug wants to distribute (lipophil) NO CLINICAL USE (other than smoking cessation) |
| hexamethonium | ganglionic blocker |
| trimethaphan | ganglionic blocker |
| mecamylamine | ganglionic blocker |
| ganglionic blockers | block all transmission through the ganglia (both SNS & PSNS) drugs very good at lowering BP (1st antiHTN) block baroreceptor SE - urinary retention, constipation, can't active BP when exercising! |
| Norepinephrine | interacts with receptors upon release from postganglionic nerves of SNS - primarily a NT, also a hormone |
| Epinephrine | interacts with receptors upon release from adrenal medulla - primarily a hormone, also a NT in CNS |
| indirect acting adrenergic | - causes release of NE/Epi - blocking reuptake** main one - inhibit metabolism |
| R-isomer catecholamine | 25x MORE POTENT than the S-isomer |
| MAO | enzyme found in GIT and synapse of noradrenergic neurons |
| COMT | enzyme found in liver and adrenergic synapse |
| NE - receptors | Alpha 1, Beta 1 |
| Epi - receptors (epi does it all!) | Alpha 1, Beta 1, Beta 2 **high dose looks like NE (effects) |
| Isopreterenol | Beta 1, Beta 2 |
| B-adrenergic agonists clinical use | - asthma and COPD (B2) - stimulating the heart (B1) - preventing pre-term labor (B2, terbutaline) |
| isopreterenol | NON-selective B agonist can cause tachycardia, not selective enough to avoid SEs |
| metaproterenol | B2 SELECTIVE agonist - short acting |
| albuterol (Ventolin, Proventil) | B2 SELECTIVE agonist - short acting |
| terbuatline (Brethine) | B2 SELECTIVE agonist - short acting |
| salmeterol (Serevent) | B2 SELECTIVE agonist - long acting |
| formoterol (Foradil) | B2 SELECTIVE agonist - long acting |
| side effect of B2 agonists | TREMORS! bc of receptors in skeletal muscle - decreases with time due to desensitization of receptors (be careful with this though!) TACHYCARDIA! due to a small amt of B2 receptors in the heart or indirectly due to baroreceptor (bc lowered BP) |
| A1-agonists clinical use | systemic - tx for severe cases of HYPOtension, usually during surgery local - reduce bleeding at a surgical site - in eye to get red out! - decongestant (decr fluid to nose) |
| tetrahydrozaline | A1-agonist for red eye |
| naphozoline | A1-agonist decongestant |
| A2-agonist | decrease presynaptic release of NE - could lower BP bc less vasoconstriction |
| clonidine | A2-agonist - probably acts in CNS to produce anti-HTN effect |
| amphetamine | INDIRECT acting adrenergic - increases release of NE (relies on a storage of NE already present) |
| methamphetamine | INDIRECT acting adrenergic - increases release of NE (relies on a storage of NE already present) ** longer duration of actino due to steric hindrance to MAO, also more lipophilic brain quicker |
| cocaine | INDIRECT acting adrenergic - reuptake inhibitor (of NE, Epi, and dopamine) can only have an effect when neuron is firing - can increase BP!!! |
| ephedrine | MIXED acting adrenergic - release and at receptors - threo isomers (opposite) - more dramatic effect on HR, BP, and CNS excitation than pseudo - constricts urinary sphincter - can cause bronchodilation (good) |
| pseudoephedrine | MIXED acting adrenergic - predom indirect though, release - erythro isomers (same) |
| ephedrine contraindication | BPH!! this and psuedo alkaloid from plant "Ma Huang" |
| phentolamine | NON-selective Alpha antagonist - increased release of NE (A2 lock) - vasodilation (A1 block) --> can lead to reflex tachycardia not used any more |
| phenoxybenzamine | NON-selective Alpha antagonist - increased release of NE (A2 block) - vasodilation (A1 block) --> can lead to reflex tachycardia not used any more |
| prazosin (Minipress) | Alpha 1 ANTAGonist - 1000x more potent at A1 than A2 for HTN and BPH vasodilates venous BV to decr venous return and CO, may decr TPR - may have effect in CNS (inhibit baroreflex) CAUTION - first dose syncope (50%) can also cause conge |
| terazosin (Hytrin) | Alpha 1 ANTAGonist - similar profile to prazosin one added benefit for BPH: causes apoptosis in prostate cells (in addition to the A block) |
| doxazosin (Cardura) | Alpha 1 ANTAGonist - similar profile to prazosin one added benefit for BPH: causes apoptosis in prostate cells (in addition to the A block) |
| alfuzosin (Uroxatral) | Alpha 1 ANTAGonist - NOT approved for antiHTN but for BPH (can offlabel though) acts similarly as the other zosins |
| tamsulosin (Flomax) | Alpha 1 ANTAGonist --> selective antag for prostate receptors! (A1a) - used ONLY for BPH (minimal effect on blood pressure) |
| silodosin (Rapaflow) | Alpha 1 ANTAGonist --> selective antag for prostate receptors! (A1a) - used ONLY for BPH (minimal effect on blood pressure) |
| yohimbine | Alpha 2 ANTAGonist - increase release of NE (A2 block) increases outflow from SNS and potentiates NE actions by blocking negative feedback - old wives tale tx for ED but no evidence |
| non selective B blockers | can cause life threatening bronchoconstriction in asthma and COPD patients (although B-blockers have little effect on respiratory func in normal people) |
| pushing a dose of selective | lose the selectivity the higher you push the dose |
| propanolol | NON-selective B blocker (1st gen BB) |
| pindolol | NON-selective B blocker (1st gen BB) has Intrinsic Sympathomimetic Activity - not clear if this is an advantage |
| metoprolol (Lopressor) | Beta 1 ANTAGonist (2nd gen BB) |
| atenolol (Tenormin) | Beta 1 ANTAGonist (2nd gen BB) |
| labetolol (Normodyne) | NON-selective B blocker & A1 ANTAG (3rd gen BB) an additional CV effect bc of l |
| carvedilol (Coreg) | NON-selective B blocker & A1 ANTAG (3rd gen BB) an additional CV effect bc of alpha BUT now back to nonselective |
Created by:
astephens5
Popular Pharmacology sets