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101 Cards in this Set
- Front
- Back
- 3rd side (hint)
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Theophylline
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inhibits phosphodiesterase
prevents cAMP-->5'-AMP -bronchodilator (not used anymore) -used for asthma |
ADVERSE EFFECTS
-seizures -poss. fatal arythmias |
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Caffine
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prevents phosphodiesterase
no cAMP-->5'-AMP -asthma treatment -relax sm. muscle of bronchioles |
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Papaverine
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prevents phosphodiesterase
no cAMP-->5'-AMP |
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Sildenafil
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prevents cGMP-->5'GMP
-increase sm. muscle relazation and blood flow to corpus cavernosa -treat impotence |
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Pilocarpine
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Muscarinic AGONIST
not metabolized by Achase or pseudoAchase -contraction of meridional fibers of ciliary muscle -increase AH flow/ decrease IOP ADVERSE EFFECTS: -poor night vision -impairs far vision CONTRAINDICATIONS -asthma and COPD -hyperthyroidism (atrial flutter) -dialated heart (atrial flutter) -peptic ulcer |
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Contraindications of Pilocarpine
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-asthma and COPD
-peptic ulcers (too much stomach acid) -hyperthyroidism (AFib) -dialated heart (AFib) |
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MOA Pilocarpine
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-Muscarinic agonist
-contracts meridional fibers of the ciliary body -increase AH flow -decrease IOP |
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MOA Trimethapham
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blocks the N1 nicotinic receptors
will block both PS and S effects -produce controlled hypotension during head and neck surgeries -release histamine for further vasodilation IV |
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MOA Mecamylamine
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blocks the N1 nicotinic receptors
will block both PS and S effects -produce controlled hypotension during head and neck surgeries -release histamine for further vasodilation PO |
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MOA Tilolol
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Beta ANTAGONIST
blocks B rec. decrease secretion of AH decrease IOP |
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Adverse effects Timolol
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-Systemic absorption
-bronchoconstriction (B2 antagonist) -bradycardia |
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Latanoprost
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stable analog of PGF2a
increase uveosclereal flow -lowers IOP |
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Bimatoprost
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stable analog of PGF2a
increase uveoscleral flow -increase length and thickness of eyelashes |
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Ephedrine MOA
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direct effects on B rec.
indirect stimulation on a rec. via increased systemic NE WILL ONLY WORK IF SYMPATHETIC INTACT |
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Phenylephrine
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direct stimulation of a1 rec.
will work with or without sympathetic stimulation |
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Carbachol MOA
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N and Musc. rec. agonist
slow onset of miosis -used to cause miosis after surgery |
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Isofluophate (DFP) MOA
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AChase inhibitor
lower IOP by increasing ACh in cleft "last resort drug"--> cataracts and general toxicity (given locally) |
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Change a 3 amine to a 4 amine will-->
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decrease lipid solubility
decrease oral bioavailability decrease x to placenta, eye, and brain |
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AChase inhibitors- carbamate
4' amines |
Neostigmine
Edrophonium (Tensilon) Pyridostigmine- long-term MA p.o. therapy |
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Dimpylate
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AChase inhibitor- organophosphate
used as garden/lawn insecticide |
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Edrophonium
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Tensilon
carbamate AChase inhibitor diagnostic for MA vs. cholinergic crisis for those on PYRIDIOSTIGMINE |
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Pyridiostigmine
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carbamate AChase inhibitor
4' amine long-term p.o. MA therapy |
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Cyclopentate
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musc. rec. antagonist
not for NARROW-ANGLE GLAUCOMA |
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N-methylatropine
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4' amine
musc. ANTAGONIST |
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GLYCOPYRROLATE
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4' amine
musc. antagonist peri-op. use to increase HR and decrease secretions |
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4' amines
musc. antagonists |
N-methylatropine
Methscopolamine Glycopyrrolate Ipratropium Tiotropium |
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Benzotropine
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3' amine
musc. rec. ANTAGONIST spec. for CNS |
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Last resort drugs for glaucoma
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Isofluophare
Echothiophate -general toxicity -cataracts |
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Betaxolol and Timolol
S/E |
-bradycardia
Betaxolol (B2) less effective Timolol (B1) bronchoconstricion |
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Dorzolamide
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carbonic anhydrase inhibitor
Tx Glaucoma S/E = urinary frequency |
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Pilocarpine S/E
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-AFib (hyperthyroidism)
-asthma and COPD bad -peptic ulcers bad |
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Myadrisis during fundoscopic examination
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Tropicamide
Cyclopentate DOC refractive error exam |
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Myadriasis during refractive error exam
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Cyclopantate DOC
Topicamide = fundoscopic |
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Glycopyrrolate
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4' amine
musc. rec. ANTAGONIST peri-op decrease secretions and reverse bradycardia |
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pralidoxime
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increase hydrolysis of P on AChase from organophosphates
OD on organophosphates |
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OD carbaryl
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atropine only
3' amine AChase inhibitor |
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Ipratropium
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4' amine
musc. antagonist REALX BRONCHIAL SM. MUSC. |
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Edrophium
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Tensilon
4' amine AChase inhibitor- carbamate |
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4' amine
AChase inhibitor carbamate |
Edrophium
Neostigmine Pyridostigmine |
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Pyridostigmine
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4' amine
AChase inhibitor-carbamate long-term MA therapy |
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Trihexaphenidyl
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3' amine
musc. rec. ANTAGONIST TORTICOLLIS |
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ACh agonist spec. GI/GU
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bethanechol
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Phyostigmine
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3' amine- many CNS SE
AChase inhibitor -Alzheimers (old drug) -OD on antichoinergic drugs |
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Donepezil
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Alzheimers DOC
carbamate AChase inhibitor 3' amine |
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Alzheimer's drugs
3' amines AChase carbamate |
Phyostigmine
Donepezil Rivastigmine Galantamine |
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DOC Alzheimers
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Donepezil
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Phyostigmine uses
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-Alzheimers (old drug)
-OD on anti-cholinergic drugs (3' AChase inhibitor- carbamate) |
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Echothiophate
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OP AChase inhibitor
last resort drugs |
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TARGET: EPINEPHRINE
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B2 > B1 > a (agonist)
sm. dose diff. from lg. dose |
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TARGET: Phenylephrine
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a1 agonist
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TARGET: Norepinephrine
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a1 agonist
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TARGET: Isoproterenol
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B1 = B2 agonist
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TARGET: Dopamine
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D1 > B1 > a1 (agonist)
3x dose changes |
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TARGET: Dobutamine
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B1 > B2 (agonist)
(+) enantionmer blocks a1 |
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TARGET: Tertbutaline
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B2 > B1 (agonist)
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TARGET: Albuterol
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B2 > B1 (agonist)
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TARGET: Salmeterol
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B2 > B1 (agonist)
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TARGET: Ritodrine
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B2 > B1 (agonist)
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TARGET: Oxymetazoline
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a only
(agonist) |
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Benefits: Dobutamine vs. Dopamine
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DOBUTAMINE=
-less likely to cause tachycardia -no change on DBP/TPR -venous dilation eases strain on ventricular wall = prevent further ischemia |
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Dopamine and MI
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large doses=
increase TPR/ DBP increase wall tension increase O2 demand further ischemia more likely to cause tachycardia |
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Tx: Ritodrine
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relax uterus for pre-term or breech
B2>B1 |
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Salmaterol
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B2 > B1
bronchodilator for asthama/ COPD/ bronchitis |
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Albuterol
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B2 > B1
bronchodilator for asthama/ COPD/ bronchitis |
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Tertbutadine
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B2 > B1
bronchodilator for asthama/ COPD/ bronchitis |
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COMT
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breaks down catecholamines-
methylation of hydroxyl on ring in CYTOSOL of most cells |
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MAO
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in MITOCHONDRIA of hepatocytes and neurons
deaminates terminal amine |
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Dobutamine Tx
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-increase CO for MI pts.
-BP > 70-100 and no signs of shock -B1 > B2 -increase dp/dt, SV, PP -no change TPR/DBP |
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MOA: Dobutamine
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B1 > B2
-increase dp/dt, SV, PP -no change DBP/ TPR |
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using Dobutamine with Dopamine
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DOBUTAMINE (+) enantiomer blocks a1-rec.
will counter vasoconstriction with dopamine prevents further ischemia in MI pts. |
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rate limiting step in NE/EPI formation
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L-tyrosine -----> L-DOPA
-enzyme = tyrosine hydroxylase - NE (-) feedback |
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Intermediates for NE/EPI formation
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L-tyrosine
L-DOPA L-dopamine L-NE L-EPI |
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PNMT
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converts NE to EPI
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Dopamine: small dose
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hits D1
increase flow to renal afferent arterioles increase RBF/ GFR/ Na+ clearance |
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Dopamine: medium dose
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hits D1 and B1
(in addition to increased RBF) myocardium stimulated increase CO/ SV further increase RBF/ GFR/ Na+ clearance |
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Dopamine: high dose
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D1, B1, and a1 hit
vasoconstriction occurs increase afterload/ TPR/ DBP |
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Afterload impact with MI
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afterload decreases substantially
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DOC Anaphylaxis
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Epinephrine
B2 > B1 > a also glaucoma |
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DOC priaprism
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low leves cause a1 corpus cavernosa relaxation
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Tyramine MOA
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indirect adrenergic agonist
increase NE release |
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Indirect Adrenergic Agonists
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Pseudoephedrine - also direct B1/B2
Ephedrine- also direct B1/B2 Amphetamine Tyramine |
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Phenoxybenzamine
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(+++) a1 antagonist
(+) a2 antagonist |
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Phenoxylbenxamine MOA
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(+++) a1 antagonist
(+) a2 antagonist |
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Phentolamine
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a1 = a2 antagonist
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Phentolamine MOA
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a1 = a2 antagonist
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Prazoin
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a1 only (ANTAGONIST)
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Labetalol
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a1 only (ANTAGONIST)
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a1 only antagonists
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Prazoin
Labetalol Tamsulosin (a1a only) |
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a1a antagonist only
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Tamsulosin
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Tamsulosin
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a1a antagonist only
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Yohimbine
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a2 antagonist (+++)
a1 antagonist (+) |
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target a2 antagonist
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Yohimbine
will alse hit a1 to a much lesser extent |
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Ergotamine
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partial a-antagonist
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Dihydroergotamine
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partial a-antagonist
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Ergonovine
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partial a-antagonist
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Methtylergonovine
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partial a-antagonist
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post-partum hemorrhage
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ergonovine
methylergonovine (partial a-antagonists) |
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treatment for migraines
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ergotamine
dihydroergotamine (partial a-antagonists) |
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Tx: Phenoxybensamine
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-control BP w/ malignant tumors
(a1 > a2 antagonists) |
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Tx: Prazosin
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-peri-op BP control
-Raynoud's syndrome -frost-bite -vascular spasm (a1 only) |
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Tx: Labetolol
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-slowly lower BP in hypertensive crisis
(a1 only) |
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