Pharmacology Flashcards
(29 cards)
Cholinesterase inhibitors
prolong ACh, which acts on the parasympathetic nervous system –> can be used a poison (shortest acting - alcohols, longest acting, organophosphates *aging)
Nicotine
nAch receptors tend to desensitize at neuromuscular junction
Muscarine
Mimics function of ACh in muscarinic part of cholinergic NS
Atropine
Competetive muscarinic ACh antagonist –> block binding sites for ACh “dry as a bone, blind as a bat, red as a beet, mad as a hatter”
Scopolamine
Muscarinic cholinergic antagonist (blocks PS) dilated eyes
Neostigmine
Interferes with breakdown of ACh, stimulates muscarinic and nicotinic
Pralidoxime
Antidote to AChE inhibitors, antagonize mAChR receptors and inhibit esterase inhibtor (cannot reach CNS) “chemical crowbar” with short time window due to aging
Amphetamine
Indirect agonists: increase transmitter in synapse by promoting release
Phenylephrine
Adrenergic agonist Alpha1 - increase peripheral arterial resistance and decrease venous capacitance, nasal decongestant
Pseudoephedrine
Adrenergic - indirect agonist, presynaptic NE releasing agent, nasal decongestant
Cocaine
NE reuptake blocker
Clonidine
Adrenergic agonist Alpha2 - antihypertensive
Prazosin
Alpha1 antagonist: hypertension
Propranolol
prototype Beta1/2 blocker: hypertension, angina, arrythmias, migraine, anxiety
Tyramine
Tyramine (wine, cheese, chocolate) leads to NA release, increase in BP
Parasympathetic system
Organs of head, neck, trunk & external genitalia;
Cardiac and smooth muscle; gland cells; nerve terminals ACh Muscarinic
Sympathetic
Organs of head, neck, trunk & external genitalia, sweat glands, adrenal medulla, arrector muscles of hair, all vascular smooth muscle
Sweat glands Muscarinic; cardiac and smooth muscle, gland cells, nerve terminal (all adrenergic - Alpha/Beta), renal vascular smooth muscle (dopamine)
Catecholamine biosynthesis
Tyrosine –> DOPA –> Dopamine –> Norepinephrine –> Epinephrine
Important Muscarinic receptors
M1 postganglionic neuron
M2 heart
M3 exocrine
Difference between muscarinic and nicotinic receptors
M - g-protein coupled receptor, much slower than N which is a ligand gated ion channel
Liver P450
Liver enzymes deactivate some drug molecules; P450 genetically determined, some lack CYP activities others have higher
HPA Axis
Hypothalamus - sends neuropeptide (pituitary portal system) –> anterior pituitary - sends protein/peptide hormone (systemic circulation) –> Target organ
Cortisol production
Paraventricular Nucleus (PVN) - sends Corticotropin releasing hormone –> Coriticotrope cell - sends ACTH (product of POMC, cleaved) –> Adrenal Cortex
Where is cortisone produced in adrenal cortex?
Zone resticularis and fasiculata