Pharm Flashcards
First order kinetics
Constant fraction
1/2 life’s
Weak acids
Cations Na, K
Propofol and barbs
Weak bases
Anions Cl-
Locals, opioids
Blood gas partition coefficients
Halothane- 2.5 This is saying 2.5:1 or 250:100 parts in
ISO- 1.46 Blood over gas.
Sevo- 0.65 He is doing nothing, most to least soluble
Des- 0.42
Nitrous- 0.46
Vapor pressures
Sevo- 170
Enflurane- 175
ISO- 240
Halo- 243
A1 agonist
Increases CA+ causes muscle contraction
Phenylephrine
A2 agonist
Inhibits adenylate cyclase which limits exocytosis of norepinephrine, in the CNS produces sedation and reduced sympathetic outflow leading to peripheral dilation and decrease BP.
Clonadine
Beta 1 agonist
Activate adenylate cyclase➡️ATP to cAMP➡️positive chrono, ino, dromotrophic effects.
Beta 2 agonist
Activates adenylate cyclase and promotes smooth muscle relaxation, gluconeogenesis, and insulin release
Promotes:
Hyperglycemia, hypokalemia.
Alpha 1 Antagonist
Prazosin
Alpha 2 antagonist
Yohimbine, used to treat impotence
Beta antagonist
“OLOL”
A-M= beta 1
N-z= beta 2. ( with beta 2 blockade K+ levels increase)
What drug class inactivate acetylcholinesterase and plasma cholinesterase? Examples?
Cholinesterase inhibitors
Reversal agents
Cholinesterase inhibitor used to diagnose myasthenia gravis
Edrophonium, short acting, electrostatic bonds.
Give up to 10mg, if increased weakness it cholinergic crisis, if symptoms improve implies its myasthenia gravis.
Neostigmine and pyridiostigmine
Covalent bond, also direct agonist effect on nicotinic receptors
Antilirium?
Physostigmine, tertiary amine, crosses BBB, used to treat anticholinergic toxicity caused by antimuscarinic overdose.
Echothiopate
Cholinesterase inhibitor
Irreversible bond, used to treat glaucoma
Can cause prolong SUCCS and mivacurium blockade bc pseudo cholinesterase inhibition.
Cholinergic syndrome/crisis
Physostigmine or organic insecticide can produce symptoms of excessive acetylcholine
Miosis, salivation, Brady, bronchoconstriction, confusion, seizure
Tx with atropine
Cholinergic crisis cause by ANTICHOLINEesterase drug.
Class of drugs that combine with muscarinic receptors and prevent acetylcholine from attaching to receptors. Examples
Antimuscarinic- atropine, glyco, scopolamine.
Most Tachy- atropine
Least sedation- glyco
Anticholinergic syndrome
Response to high dose atropine or scopolamine.
Tachy, excitation, agitation, dry and flush skin
Tx with physostigmine
Anticholinergic syndrome caused by an ANTIMUSCARINIC.
Myasthenia gravis
Autoimmune Destruction of post synaptic acetylcholine receptors
Causing weakness, fatigue of skeletal muscle
Tx with Anticholinesterases, unknown response to succs, but very SENSITIVE to NDMB
Myasthenic crisis
Acute exacerbation of myasthenia gravis
Characteristics of muscle relaxants
100% ionized at PH Highly protein bound Do not cross BBB or Placenta Trapped in renal tubule bc of ionization All can be excreted in kidney if other routes unavailable
Muscle relaxation and disease
Disease that cause increase in ACH RECEPTORS such as muscle denervation injury make the patient sensitive to SUCCS but bc more receptors require increase dose of NDMB.
Dsease like myasthenia decrease receptors so the opposite is true.
Long acting NDMR
PGP- MD
Pancuronium,gallamine, pipecuronium
Metocurrarine, d-tubocurarine
Intermediate acting NMB
Vec and roc
Short acting
Miv
Atra
And cistatracurium
Renal excretion primary route
All long acting
PGP-MD
Biliary Excretion primary route
Vec and roc
METAbolism primary route of elimination
Succs- pseudocholinesterase
Mivacurium- plasma cholinesterase
Atracurium- ester hydrolysis and hoffman
Cistatracurium- Hoffman
Relaxants with histamine release
DAMMS d-tubo Atra Mivacurium Metocurarine Succs
Relaxants with Autonomic blockade
MD
Metocurarine
D-tubo
Relaxants with bradycardia
Succs
Relaxants with tachycardia
Reflex- MAD
Metocurarine, atra, d-tubo
Antimuscarinic-
Pancuronium
Gallamine
Hypotension from NMB
Succs, d-tubocurarine, metocurarine
Hypertension from NMB
Pancuronium and Gallamine
Opioid receptors
Mu1- euphoria, pruitus, low abuse, supraspinal
Mu2- resp depression, dependence, constipation, spinal analges
Kappa- dysphoria, sedation, low abuse potential
Delta- resp depression, dependance, constipation
Opioid agonist/antagonist
Nubaine, stadol
Work on kappa and delta
Zero order kinetics
Constant amount (2mg per min)
Alcohol, Asa, phenytoin