Sweatman Miscellaneous Drugs Flashcards
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