Third test Flashcards
Acebutolol
B1 selective blocker
Partial Agonist (ISA)
Membrane stabilizing
low lipid solubility ?
Atenolol
B1 selective blocker
Not Partial agonist
Not membrane stabilizing
low Lipid soluble
Esmolol
B1 selective blocker Not partial Agonist Not Membrane stabilizing Low Lipid Soluble rapid action, rapid broken down by plasma esterase's
Metoprolol
B1 Selective blocker
Not partial Agonist
Membrane Stabilizing ?
Moderate Lipid Soluble
Nadolol
B1 and B2 blocker Not partial agonist no membrane stabilize Low Lipid solubility longest activity
Pindolol
B1 and B2 selective blocker Partial Agonist (ISA), Membrane stabilizer ? ISA doesn't affect B2 mediated inhibition, actually enhances the relax adding to anti HTN effect Moderate Lipid soluble
Propranolol
B1 and B2 selective blocker
no partial agonist
Membrane stabilize
High Lipid soluble
Timolol
B1 and B2 selective blocker no partial agonist no membrane stabilize Moderate lipid solubility used in glaucoma treatment
PheNoxybenzamine
Non- selective a1 a2 blocker
non- competitive inhibition via Irreversable inactivation of receptor
used to prevent severe HTN episodes in pheo patients prior to surgery
better than selective a1 info b/c blocked the extra synaptic a2 in HTN
SE: inhibit some non adrenergic receptors (H, 5HT, Ach)
SE: miosis, drowsiness, vomit lethary (enters CNS), shock/circ fail
PheNtolamine
short acting a1 and a2 reversible blocker
Pheo diagnostic testing, and during surgery
used to reverse systemic vasoconstrict and related HTN from non specific a-agonist like NE
limit local dermal tissue necrosis after a-agonist injection
dental anesthetic reversal
SE: Nausea,vomit, diarrhea, Increase GI motility(bad for ulcers), may interact with non a receptors
PrazoSin
Prototype selective a1 blocker- competitive
long term treatment of mild to moderate HTN
Relax smooth muscle of bladder neck, relieve urinary obstruction
raynauds treatment
SE:First dose phenomenon orthostatic HypoTN, Na H20 retention, reflex tachycardia, not as much as non selective
DoxazoSin
newer selective a1 blocker than prazosin
use and side effect just life Prasozin, but with longer half lives so better long term control of HTN and BPH
Relax smooth muscle of bladder neck, relieve urinary obstruction
raynauds treatment
SE:First dose phenomenon orthostatic HypoTN, Na H20 retention, reflex tachycardia, not as much as non selective
TerazoSin
newer selective a1 blocker than prazosin
use and side effect just life Prasozin, but with longer half lives so better long term control of HTN and BPH
Relax smooth muscle of bladder neck, relieve urinary obstruction
raynauds treatment
SE:First dose phenomenon orthostatic HypoTN, Na H20 retention, reflex tachycardia, not as much as non selective
TamsuloSin
Selective a1 subunit A blocker(a1A)
the main subtype found in the bladder neck and the prostate vs the a1 found systemically
good drug for BPH with less systemic side effects(decrease BP, orthostatic syncop)
can still cause abnormal ejaculation
SilodoSin
Selective a1 subunit A blocker(a1A)
the main subtype found in the bladder neck and the prostate vs the a1 found systemically
good drug for BPH with less systemic side effects ( decrease BP, orthostatic syncop)
can still cause abnormal ejaculation
AlfuzoSin
selective a1 blocker used in BPH treatment but not subtype specific like tamsulosin and silodosin
shows uroselectivity by accumulating in the prostatic tissue
doesn’t significantly influence vascular alpha receptors
Reserpine
Peripherally acting Sympathetic neuronal blocker
decreases the availability of NE to its receptor by inhibiting NE and DA storage in vessicles
Guanethidine
Peripherally acting Sympathetic neuronal blocker
decreases the availability of NE to its receptor by inhibiting NE and DA storage in vessicles and preventing release
Centrally acting Sympathetic neuronal blockers
Methyldopa
Clonidine
Guanabenz
Guanfacine
methyl dopa
centrally acting adrenergic neuronal inhibitor
converted to alpha-methylNE thats acts as an a2 agonist in central vasomotor centers to dampen simp outflow leading to decreased renin, decreased HR and CO(or not), and most important decreased arterial peripherial pressure
SE:peripheral fluid retention, centrally mediated dry mouth, certain autoimmune disorders, hemolytic anemia, abnormal liver function
Clonidine
centrally acting adrenergic neuronal inhibitor
not a prodrug
similar action to methyl dopa as a a2 agonist to dampen simp outflow
lower doses than methyldopa, in patch form
no autoimmune SE, rebound HTN
treatment of: adhd, meno hot flash, stress disorder, nicotine and ethos withdrawal
Guanabenz
centrally acting adrenergic neuronal inhibitor
similar to clonidine binds a2 receptors to dampen symp outflow and treatment of HTN
shown to lower cholesterol,
less reactive fluid retention so no diuretic needed to preserve HTN effect
Guanfacine
centrally acting adrenergic neuronal inhibitor
similar to clonidine in action and HTN effect
less sedation, less likely to cause withdrawal syndrome
recently made into intuniv for ADHD
Nicotine
Ganglionic Stimulant
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