Pharm exam #2 Flashcards
Sympathetic Activity of β1
Renin release.
Accelerates SA node.
Increases heart contractility.
Relaxes skeletal blood vessels.
Sympathetic Activity of β2
Relax GI smooth muscle wall. Relax bladder. Glycogenolysis (glycogen converted to glucose) in liver. Accelerates SA node. Increases heart contractility. Relax bronchiolar smooth muscle.
Sympathetic Activity of α1
Contract smooth muscle vessels.
Glycogenolysis in liver.
Contract GI sphincter.
Contract urinary sphincter.
Sympathetic Activity of α2
Contract smooth muscle vessels.
Glycogenolysis in liver.
Relax wall of GI smooth muscles.
Parasympathetic activity of M2
Decelerates SA node.
Decreases heart contractility.
Parasympathetic activity of M3.
Relax smooth muscle of blood vessels. Contract bronchiolar smooth muscle. Contract wall of GI smooth muscles. Relaxt GI sphincter. Increase GI tract secretions. Contract bladder. Relax urinary sphincter.
SNS origin of fibers
Thoracolumbar region of spinal cord
SNS length of fibers
Short pre-ganglionic and long post-ganglionic; Has chain ganglion that can effect multiple effector organs with one stimulus
SNS Location of ganglia
Close to the spinal cord
PSNS origin of fibers
Brain and sacral spinal cord; craniosacral
PSNS length of fibers
long preganglionic and short postganglionic
PSNS location of ganglia
in the visceral effector organs
Acetylcholine
Direct cholinomimetic (parasympathomimetic).
Ester of choline. Made from acetyl Coa and choline, formed by CHAT (Choline acetyl transferase).
All pre-ganglia release this.
Permanently charged, so insoluble in lipids. Has to be given injected bc it cannot be absorbed very easily.
Miosis (pupillary constriction, short term- metabolism is 5-20 seconds), decreases IOP, (Binds to M1 sphincter receptor on eye); Contraction- prolonged can cause flaccid paralysis (On Nm of NMJ)
Methacholine
Direct cholinomimetic (parasympathomimetic).
Ester of choline (poor absorption & distribution in CNS).
Permanently charged, so insoluble in lipids. Has to be given injected bc it cannot be absorbed very easily.
Dx of asthma.
Sticks around (3x) longer than Ach bc it is not broken down as readily by enzymes.
Carbachol
Direct cholinomimetic (parasympathomimetic).
Ester of choline, derivative of Methacholine.
Resistant to hydrolysis
Miosis, decreases IOP (Binds to M1 sphincter receptor on eye)
Bethanechol
Direct cholinomimetic (parasympathomimetic).
Ester of choline, derivative of Methacholine.
Works on M3 receptor in GU, causes contraction of bladder, opens sphincter.
Resistant to hydrolysis.
Bladder dysfunction, GERD.
Muscarine
Direct cholinomimetic (parasympathomimetic). Less completely absorbed than other alkaloids bc it is charged. Elimination is enhanced in the kidneys by acidity.
Plant Alkaloids.
Pilocarpine
Direct cholinomimetic (parasympathomimetic).
Well absorbed. Elimination is enhanced in the kidneys by acidity.
Plant Alkaloids.
Edrophonium
Indirect cholinomimetic (parasympathomimetic).
Blocks acetylcholinesterase.
Simple Alcohol - fast duration 5-15 minutes
Acts on M3 receptor in GI; increases digestion, improves illius.
Myasthenia Gravis diagnosis
Neostigmine, Physostigmine
Indirect cholinomimetic (parasympathomimetic).
Blocks acetylcholinesterase.
Carbamates - moderate
Acts on M3 receptor in GI; increases digestion, improves illius (post op bc it out competes paralytics).
Treatment of Myasthenia Gravis, surgical paralysis reversal
Duration 0.5 to 2 hours
Echothiophate
Indirect cholinomimetic (parasympathomimetic).
Blocks acetylcholinesterase.
Organophosphates - days
Glaucoma, only useful drug to help bc the duration of action is 100+ hours compared to other drugs- it is irreversibly bound to that receptor
Atropine
Cholinoreceptor blocker (parasympatholytic)
Antimuscarinic
Plant-based alkaloid from the belladona plant or jimsomweed.
L-isomer is 100x more potent than D-isomer
Use: Organophosphate poisening (with pralidoxime), bradycardia.
Blocks nicotinic-muscarinic receptors so that they cannot lose their fluid through the canal of schlemm by relaxing cilliary muscles- so be careful with giving this with glaucoma, especially closed-angle. Also be careful with elderly men and those with a history of BPH, as atropine can prevent urination.
Scopolamine
Cholinoreceptor blocker (parasympatholytic)
Antimuscarinic
Plant-based alkaloid from henbane. Similar in chemical nature to atropine.
Use: Motion sickness.
Tropicamide
Cholinoreceptor blocker (parasympatholytic) Antimuscarinic Mydriasis (cilliary muscle dilation- what you'd use at eye doc bc duration is 1/4 of a day and not DAYS like other drugs) and cycloplegia diagnosis
Ipratromine
Cholinoreceptor blocker (parasympatholytic)
Antimuscarinic
Atrovent
Asthma
Phentolamine
Sympatholytic
Alpha Blocker
Reversible
alpha 1, alpha 2 non selective
reduces peripheral resistance, some cardiac stimulation (due to blocking of alpha 2 receptors on nerves, limiting reuptake of NE and increasing NE)
Hypertension (r/t Pheochromocytoma), cardiac stimulent
Can also be used to treat male erectile dysfunction, but only if nothing else works. Not front line for this. You could directly inject it into the penis, but that could cause priapism.
Prazosin
Sympatholytic Alpha Blocker Reversible Alpha 1 highly selective Low affinity to alpha 2 Relaxes arterial and venous smooth muscle Hypertension, BPH
Yohimbine
Sympatholytic
Alpha Blocker
Reversible
alpha 2, sexual dysfunction
Lebetalol
Sympatholytic
Alpha Blocker
Reversible
Both alpha and beta
Phenoxybenzamine
Sympatholytic
Alpha Blocker
Irreversible- non-competitive antagonist
Pheochromocytoma
Propanolol
Sympatholytic
Beta Blocker - Cardioprotective, hypertension
β1, β2
Metoprolol
Sympatholytic
Beta Blocker - Cardioprotective, hypertension
β1
Safer in diabetics
Lebetalol
Sympatholytic
Beta Blocker - Cardioprotective, hypertension
α1, β1, β2
Hypertension (preeclampsia), Pheochromocytoma
Esmolol
Sympatholytic
Beta Blocker - Cardioprotective, hypertension
β1
Surgical tachycardia (fast)
Clonidine
SNS Sympathoplegic
Methyldopa
SNS Sympathoplegic
Dexmedetomidine
Precedex
SNS Sympathoplegic
Hexamethonium
Antinicotinic, cholinoreceptor blocker (parasympatholytic)
Ganglion blocker (Nn)
Refractory hypertension
Succinylcholine
Antinicotinic, cholinoreceptor blocker (parasympatholytic) NMJ Blocker (Nm); Depolarizing Prolonged fasciculations (muscle twitches). Suxx is not broken down by achesterase, so after fasciculation occurs the muscle cannot repolarize and you will have flaccid paralysis (phase 1 block). Phase 2 block is undesirable- excessive amounts eof suxx in bloodstream, so effects are prolonged, they wont be able to breathe (bad). Duration: v short, 5 minutes Use: Main use is to facilitate intubation; also used in electroconvulsive therapy so they dont hurt themselves from muscle clenching. Side effects: muscle pain, hyperkalemia. Watch for malignant hyperthermia! (autosomal dominant disorder or gene defect on the RyR1 receptor). Tx for this is Dantrolene.
Derivatives of curare
Antinicotinic, cholinoreceptor blocker (parasympatholytic)
NMJ Blocker (Nm)
Causes flaccid paralysis
Non- depolarizing, these compete with acetylcholine.
Epinephrine
Sympathomimetic
Direct Agonist
α1, β1, β2
Treat hypotension, cardiac, respiratory
Norepinephrine
Sympathomimetic
Direct Agonist
α1, β1
Cardiac
Isoproterenol
Sympathomimetic
Direct Agonist
β1, β2
Cardiac
Dopamine
Sympathomimetic
Direct Agonist
D, β1
Dose dependent (vasodilation, Vasoconstriction, Cardiac)
Dobutamine
Sympathomimetic
Direct Agonist
β1
Cardiogenic shock
Phenylephrine
Sympathomimetic Direct Agonist α Raise bp by constricting peripheral bvs Decongestant- shrinks the blood vessels going to the nose. Treatment in the tetralogy of fallot
Midodrine
Sympathomimetic
Direct Agonist
α1
Orthostatic hypotension
Clonidine (catapres)
Sympathomimetic
Direct Agonist
α2
Hypertension, hemodynamic instability
Ephedrine
Sympathomimetic
Direct Agonist
BOTH DIRECT AND INDIRECT
decongestant
Albuterol, Salmeterol, Formoterol
Sympathomimetic
Direct Agonist
β2 Selective
Amphetamine
Sympathomimetic
Indirect Agonist
Displacement of NE, reverse NET, Block DAT- diet ,ADHD, recreational
Cocaine
Sympathomimetic
Indirect Agonist
Block NET (NE transporter back into pre-synapse), DAT (Dopamine transporter back into pre-synapse), recreational
Hydralazine
Vasodilator
Minoxidil
Vasodilator
Nitroprusside
Vasodilator
Fenoldepam
Vasodilator
Verapamil
Vasodilator; CCB
Dilatiazem
Vasodilator; CCB
Dihydropyridines
Vasodilator; CCB
Aliskiren
Angiotensin inhibitor
Captopril
Angiotensin inhibitor
ACEi
Losartan
Angiotensin inhibitor
ARB
Valsartan
Angiotensin inhibitor
ARB
Bosentan
Endothelin Receptor Antagonist
Nitroglycerin
Decrease myocardial oxygen demand by decreasing heart rate/ventricular volume/BP/contractility
Nitrate/Nitrite
Large veins- best response
Increase venous capacitance, decrease ventricular preload
NO release in vascular smooth muscle - SL
Mononitro forms (isosorbide dinitrate)
Amyl Nitrite
Onset: 1-3 minutes, duration 20-30 minutes
Neurotransmitter Classes
Esters- Ach Monoamines - Amino acid derivatives, specifically the AA tyrosine; Ne, serotonin, dopamine Amino Acids- Glutamate, GABA Purines - Adenosine, ATP Peptides- Substance P, Endorphins Inorganic gases - Nitric Oxide (NO)
Acrecholine
Alkaloid from the Patel nuts.
Very similar to nicotine, crushed and used as a psychostimulant. (Red stain in mouth).
Higher incidence of oral and esophageal CA.
Nicotine
Alkaloid, Nicotinic
Suggamadex
Instead of outcompeting atropine or other cholinoreceptor blocking agents, it traps the derivatives inside a molecular tube, making it inactive.
Nearly 100% reversal, but the drug is expensive.
Activity of D1
dilates renal blood vessels/smooth muscle