Sweatman Miscellaneous Drugs Flashcards
(25 cards)
Drugs that act in the Vasomotor of the brain
clonidine, guanbenz, ganfacine, methyldopa
Drugs that work in the sympathetic nerve terminals of peripheral tissues
resperine
Alpha 2 agonists
clonidine guanabenze ganfacine *reduce sympathetic nervous system outflow
alpha 2 agonist prodrugs
methyldopa
NE storage depletion
resperine
in tx of pheochromocytoma
metryosine–>depletion of NE
alpha and beta receptors are
GPCR’s
constant stimulation of alpha receptors by catecholamine stimulation leads to
DOWNREGULATION (endocytosis) of the alpha 2 receptors–>this does not happen in occasional –>stimulation –>loss of drug activity upon these receptors
alpha 2 receptors are
autoreceptors–>take back up NE causing inhibition of further release of NE (negative feedbacker)
what defines a heteroreceptor
expression of adrenergic alpha2 receptor in non-cholinergic tissues?
sedation, analgesia, bradycardia, hypotension caused by alpha 2 agonists caused by
agents acting on heteroreceptors in the post synaptic neuron
how do alpha 2 agonists lower BP
cross BBB and work centrally to increase flow in the periphery, while in periphery they constrict–>therefore the central impact is greater than the peripheral effect
alpha 2 agonists that cannot cross the BBB
cannot effectively lower BP
IS THERE REFLEC TACHYCARDIA WITH ALPHA 2 AGONISTS
NO, HR MAY REDUCE BC OF VAGAL STIMULATION
ARE ALPHA 2AGONISTS USEFUL IN DIABETICS
YES–>NO EFFECT ON BLOOD GLUCOSE
METHYLDOPA AND IRON CHELATORS
–>CHELATES METHYLDOPA TOO MUST SEP. DOSING INTERVAL
METHYLDOPAAND RENAL FAILURE–
MUST RAISE DOSE
ADVERSE EFFECTS OF ALPHA 2 AGONISTS
DROWSINESS–> GIVE QHS DRY MOUTH–>CARIES ABDOMINAL PAIN CONSTIPATION IMPOTENCE DEC LIBIDO
METHYLDOPA INTERFERES WITH
CAECHOLAMINE QUANTITATION -CONTRAINDICATED IN PHEOCHROMOCYTOMA
CLASS B ALPHA 2 AGONISTS
METHYLDOPA GANFACINE *MOST PERMISSIVE
drug that can be used safely in pregnancy
methyldopa–>drug of choice labetolol metoprolol nefedipine
Reserpine MOA
inhibits VMAT2 –>depletion of catecholamine in presynaptic terminals ->lost capacity to conecntrate and store NE and dopamine *no mature NE vessicles
pharmacologic sympathectomy
Reserpine causes catecholamines leak into cytoplasm and are metabolize
toxicity of reserpine
CNA–>sedation, increased suicidal rates