Pharmacology Flashcards
(159 cards)
catecholamines pass the blood brain barrier well? poorly?
very poorly
acetylcholine affects what 2 receptors
nicotinic
muscarinic
secreted by cholinergic fibers
after a threshold stimulus, liberation of Ach alters the cell membrane’s permeability
epinephrine is a direct acting catecholamine and adrenergic agonist or antagonist?
AGONIST
norepinephrine is a direct acting catecholamine that works through which receptors in the CNS?
a1, a2, b-adrenergics
dopamine (intropin) is an immediate precursor to?
acts through which 2 subtype receptors?
NE
D1 - activates adenylyl cyclase
D2 - inhibits adenylyl cyclase
serotonin (5-hydroxytryptamine) works through at least 14 subreceptors __ type neurons
tryptominergic
the major inhibitory neurotransmitter in the CNS is
GABA
opioid peptides include (3)
beta-endorphin
enkephalines
dynorphin
these 2 nts have EXCITATORY effects on neurons everywhere in the CNS
glutamate
aspartate
catecholamines are a group of
sympathomimetic compounds
these 2 catecholamines stimulate the myocardium
epi
NE
clinically, epi is for
anaphylaxis, glaucoma, asthma, vasoconstriction to prolong anesthesia
clinically, norepi causes
vasoconstriction in hypotension
CNS stimulants include
- analeptics
- xanthines
- sympathomimetic amines
- analeptics - can overcome drug-induced RESPIRATORY DEPRESSION and hypnosis [metrazol, coramine, dopram, picrotoxin, strychnine]
- xanthines - improve mental ALERTNESS, reduce urge to sleep, elevate MOOD [caffeine, theophylline, theobromine]
- sympathomimetic amines - to treat NARCOLEPSY, OBESITY, ADHD [amphetamines, methylphenidate, phenmetrazine]
__ is the only xanthine important in asthma tx, by stimulating medulla respiratory centers to cause bronchial dilation
theophylline
caffeinism occurs if you intake > __ mg caffeine per day
600-750 (10 cups)
> 1000 mg is TOXIC
caffeine stimulates the CNS unequally, with the __ being the most excited, and __ least excited
CORTEX most,
spinal cord least
the Autonomic Nervous System (ANS) is an efferent motor system that fxns independent of consciousness and controls __
automatic VISCERAL fxns required for life
drugs block or mimic ANS transmitters to clinically modify what functions?
autonomic fxns like: cardiac and smooth muscle, vascular endothelium, exocrine glands, presynaptic nerve terminals)
ANS consists of 2 parts
sympathetic nervous system - response to STRESS, fight or flight
parasympathetic - at REST, rest and digest
SYMPATHETIC NERVOUS SYSTEM FUNCTION
- epi released from adrenal medulla
- HR incr (tachycardia)
- CO, Bp, blood flows from skin and internal organs into SKELETAL MUSCLE
- energy stores are mobilized
- pupils dilate (MYDRIASIS
- bronchioles dilate
- FEAR activates ANS sympathetics -> HYPERTENSION (a1 adrenergic receptors cause arteriolar vasoconstriction)
- DECR. salivation
PARASYMPATHETIC NERVOUS SYSTEM FUNCTION
- effectors are activated as needed, does not discharge as a complete system
- Cranial nerves with PS activity = 3, 7, 9, 10
- MIOSIS (pupils constrict)
- bradycardia
- incr. salivation
4 types of drug-receptor binding
- ionic - from electrostatic attraction btw ions of opp. charge
- H bonds - btw polar (water) molecules
- Van der Waals - weak interactions when atoms close
- Hydrophobic - btw drug, receptor and aqueous environment
covalent bonds
sharing e- by pair of atoms, for structural integrity of molecules, NOT involved in drug-receptor rxns