Pharm: ANS, Autacoids, Diuretics, HTN, CHF, Angina Flashcards
H1 receptor is similar to…
M3 receptor (endothelium, smooth muscle, nerve endings) Gq
H2 receptor is similar to…
Beta-2 receptor (gastric mucosa, heart, immune cells) Gs
Low dose ACh vs. High dose ACh [barorecepror reflex]
Low dose: M3 hypotension, reflex tachycardia
High dose: M2 bradycardia
Cholinergic agnonists activating both M & N
Carbachol, arecoline
Methacholine
[M ag] Diagnosis of bronchial airway hyperactivity in patients without clinically apparent asthma
Carbachol
[M ag] Miosis; decrease IOP
Bethanachol
[M ag] Acute post-op urinary retention, neurogenic bladder
Pilocarpine
[M ag] Sialagogue, Miosis, decrease IOP
* Acute glaucoma
Edrophonium
[Anti-AChE] Diagnosis MG, reverse NM effect of non-depolarizing blocker
Physostigmine
* AE
[Anti-AChE] Trmt for OD on anti-cholinergic drugs
* Do not treat a TCA overdose patient: depress cards conduction
Neostigmine
[Anti-AChE] Stimulate bladder, antidote to competitive antagonist at NMJ, treatment MG
Pyridostigmine
[Anti-AChE] MG treatment
Echothiophate
[Anti-AChE] Glaucoma
Pralidoxime
Re-activator of AChE: must use before aging in organophosphate poisoning
Donepezil, rivastigmine, tacrine, galantamine
[Anti-AChE] Alzheimer’s treatment
Among the anti-cholinesterases, which group forms the strongest covalent bond?
Organophosphates
Atropine is contraindicated in…
What is the surgical use of atropine?
Atropine flush?
Angle-closure glaucoma, BPH, elderly
- Block respiratory secretions
- Given in high doses
Scopalamine (2 uses)
[M antag] Motion sickness
Block STM memory - anesthetic
Ipratropium & Tiotropium
[M antag] COPD & Asthma
Homatropine, Cyclopentolate, Tropicamide
[M antag] Mydriasis with cycloplegia [better than atropine, because shorter duration of action]
Benztropine & Trihexyphenidyl
[M antag] Parkinsonism & effects of anti-psychotics
Glycopyrrolate PO vs. IV
[M antag] PO: decreased GI motility; IV: prevent bradycardia during surgery
Tolterodine
[M antagonist] Overactive bladder
Hexamethonium, mecamylamine, trimethaphan
[N ganglion blockers] Reverse the dominant control, i.e. sympa reversal of arteries, veins, sweat glands [dilation/dilation/anhydrosis]
Tubocurarine
[NMJ non-depolarizing competitive antagonist] Skeletal muscle relaxation during surgery
Succynylcholine
* AE
[NMJ depolarizing blocker] Rapid intubation/ECT
* Malignant hyperthermia (excessive Ca release from SR when given with halogenated anesthetic); treat with dantrolene
Dantrolene
Treatment for anesthesia-induced malignant hyperthermia
Hemicholinium
[Pre-syn chol antag] prevents uptake of choline (CHT)
Vesamicol
[Pre-syn chol antag] prevents ACh storage [ACh-H+ antiport]
Botox
[Pre-syn chol antag] prevents ACh release [spasm/wrinkles]
Low dose epi vs. Large dose epi [baroreceptor reflex]
Low dose: no baroreceptor reflex (because B2»_space; Alpha 1)
NE
- Receptors
- Reflex brady? How to overcome?
Alpha 1, Alpha 2, Beta 1
Reflex bradycardia: pre-treat with atropine
Dopamine
* Treatment of choice for shock?
Treatment of choice for shock; prevents renal shutdown
Phenylephrine
[A1 Ag] vasoconstrictor: nasal decongestant, dilate pupil, shock, SVT
Clonidine
* AE
[Central A2 Ag] Decrease BP [lethargy, sedation, xerostomia]
Methyldopa
[Central A2 Ag] Treatment of choice for pregnancy-induced HTN
Brimodine
[Alpha 2 Ag] Glaucoma (decreases production/ increases outflow)
Isoproterenol
[B Ag] B1: increase HR; B2: dilate arterioles
Dobutamine
[B1 Ag] Acute management of CHF; increases CO without increasing HR and oxygen demand of the heart
Albuterol & Terbutaline
Salmeterol & Formoterol
* AE
Asthma short acting vs. Long action
AE: tremor, restlessness, apprehension, anxiety, tachycardia (less likely with inhaled)
Amphetmine
[NE release + potentiate NE] Increase BP
Methylphenydate
[NE release + potentiate NE] ADHD
Tyramine
[NE release + potentiate NE] Cheese/Wine metabolized by MAO – MAOI serious side effects
Cocaine
[Uptake inhibitor]
Atomoxetine
[Uptake inhibitor] ADHD
Ephedrine
[Mixed NE release/adrenergic receptor] Pressor (hypotension during spinal anesthesia); MG treatment; bronchial asthma treatment; not metabolized by COMT
Pseudoephedrine
[Mixed NE release/adrenergic receptor] OTC decongestant
Phenoxybenzamine
Phentolamine
Phenoxy: irreversible pheo
Phentolamine: reversible; STM pheo/HTN crisis; withdrawal clonidine
Epinepherine reversal?
Phenoxybenzamine/Phentolamine
Prazosin, Terazosin, Doxazosin, Tamsulosin
- First dose?
- AE?
[A1 antagnonist] BPH & HTN except tamsulosin
- First dose exaggerated response
- Orthostatic hypotension
Yohimbine
[A2 Antagonist] past treatment for ED (replaced by phosphodiesterase inhibitors)
Propranolol is contraindicated in…
[B-blocker] Asthmatics, DM (may impair recovery from hypoglycemia & mask the tachycardia associated with hypoglycemia)
Timolol
[B-blocker] Glaucoma, HTN, migraine
Why shouldn’t beta-blockers be withdrawn abruptly?
Tachycardia, HTN, ischemia 2/2 upregulation of beta-receptors
Nadolol
[B-blocker] Longer duration of action; Angina/HTN
Atenolol, metoprolol
* AE
[B1-Antag] HTN patients with impaired pulmonary function; DM patients on insulin/oral hypoglycemic
* Still avoid in asthmatics b/c beta-2 effects
Esmolol
[B1-Antag] 1/2 life 10 minutes: SVT, thyrotoxicosis, peri-operative HTN, myocardial ischemia in acutely ill patients
Labetalol, Carvediol
[A1 & beta blockers] HTN, HTN/CHF
Pindolol
[Partial agonist] HTN in pts with impaired cardiac reserve and a propensity for bradycardia
Metyrosine
Competitive inhibitor of tyrosine-hydroxylase; malignant pheo/perioperative management
Reserpine
Damages VMAT irreversibly; no storage of NE/dopamine in vesicles
Guanethidine
Displaces NE from vesicles; inhibits release of NE
Cromolyn, Nedocromil
Histamine release inhibitor
Fexofenidine
Second generation H-1 antagonist (less sedative side effects 2/2 increased lipophilicity)
Loratidine
Second generation H-1 antagonist (less sedative side effects 2/2 increased lipophilicity)
Cetrizine
Second generation H-1 antagonist (less sedative side effects 2/2 increased lipophilicity)
Cimitidine
* AE
H-2 antagonist [inhibit gastric acid secretion – peptic ulcer, acute stress ulcer, GERD]
Inhibits CYP450, Anti-Androgen; IV/ICU can induce renal/hepatic dysfunction
Ranitidine
[Zantac] H-2 antagonist [inhibit gastric acid secretion – peptic ulcer, acute stress ulcer, GERD]
Famotidine
[Pepcid AC] H-2 antagonist [inhibit gastric acid secretion – peptic ulcer, acute stress ulcer, GERD]
Nizatidine
H-2 antagonist [inhibit gastric acid secretion – peptic ulcer, acute stress ulcer, GERD]
Chlorpheniramine
First generation H-1 antagonist; Allergies, motion sickness, somnifacents
Cyclizine
First generation H-1 antagonist; Allergies, motion sickness, somnifacents
Diphenhydramine
First generation H-1 antagonist; Allergies, motion sickness, somnifacents