vascular system rx Flashcards
pul HTN med classes
endothelin receptor antag
PDE5 inhibitors
prostacyclin analogues
Soluble guanylate cyclase stimulator
Prostacyclin receptor agonist
Endothelin receptor antagonists names
Ambrisentan
Bosentan
Macitentan
all available as PO form
Endothelin receptor antagonists MOA
Block the ETA and ETB receptors- but have a high affinity for ETA
Ambrisentan
Bosentan
Macitentan
ADRs of ERA’s
Peripheral Edema
Headache
Dyspepsia
Flushing
Liver dysfunction (more common with bosentan)
dental implacation of ERA’s
gum bleeding
PDE5 inhibitor names
available as?
Sildenafil
Tadalafil
Available: PO
PDE5 inhibitors MOA
Inhibits action of phosphodiesterase 5 (PDE5), increasing intracellular cGMP concentrations, lowering
the intracellular Ca++ concentrations, resulting in vascular smooth muscle relaxation
Sildenafil
Tadalafil
PDE5 inhibitors ADRs
Flushing
Headache
Dyspepsia
Skin rash
PDE5 inhibitors dental
Avoid nitrate use
Prostacyclin analogue names
and forms
Epoprostenol: Available: IV
Iloprost: Available: Inhalation (Inh)
Treprostinil: Available: PO, Inh, IV, and SQ
prostacyclin analogues MOA
Binds to prostacyclin receptor (IP), stimulate
activity of adenylate cyclase (AC), increases intracellular cyclic AMP levels, lowering the intracellular Ca++ concentration, resulting in vascular smooth muscle relaxation
prostacyclin analogues ADRs
Jaw Pain (dose limiting)
Platelet inhibition (increased bleeding)
Headache
Flushing
Hypotension
Infusion site pain
prostacyclin analogue dental
Increased risk of bleeding due to platelet inhibition
Jaw pain (dose related ADR)
Soluble guanylate cyclase stimulator
name and form?
Riociguat
Available: PO
Soluble guanylate cyclase stimulator moa
Sensitizes guanylyl cyclase to nitric oxide but also
directly activates guanylyl cyclase, increasing intracellular cGMP concentration, lowering the intracellular Ca++ concentration, resulting in vascular smooth muscle relaxation
Soluble guanylate cyclase stimulator ADRs
Hypotension
Dyspepsia
Headache
Edema
Soluble guanylate cyclase stimulator dental
Increased risk of bleeding=
Risk of unanticipated bleeding during procedure
prostacyclin receptor agonist name/form
Selexipag
Available: PO
Prostacyclin receptor agonist moa, name?
Selective IP receptor agonist, stimulate activity of adenylate cyclase (AC), increases intracellular cyclic AMP levels, lowering the intracellular Ca++ concentration, resulting in vascular smooth muscle relaxation
Selexipag
Prostacyclin receptor agonist ADRs
Jaw pain
Flushing
Headache
Skin rash
Diarrhea
prostacyclin receptor agonist dental
Jaw pain (~1 in 4 patients)
Direct Acting Vasodilators names/ forms?
Minoxidil (PO)
Sodium Nitroprusside (IV only)
Hydralazine (IV and PO)
Minoxidil MOA
Causes smooth muscle relaxation by opening KATP channels. Primary effects on arteriolar smooth muscle,
with little to no effects on veins.
Minoxidil ADRs
Hair Growth
Edema
Photosensitivity (rare)
Hypotension
Minoxidil dental
ortho hypo
Na nitroprusside MOA
Direct donates a NO molecule, which activate guanylate
cyclase (GC) to increase cGMP resulting in smooth muscle relaxation. Does not require ALDH2. Does not exhibit tolerance
Na nitroprusside ADRs
Severe hypotension, flushing, reflex tachycardia, methemoglobinemia, thiocyanate toxicity.
Thiocyanate can form in the parenteral fluid due to exposure to light, product MUST BE PROTECTED form
light. This is more common with higher doses and longer durations of administration.
Hydralazine MOA
Direct acting vasodilator thru interference with action of IP3 on calcium release from sarcoplasmic reticulum.
Primary effects on arteriolar smooth muscle, with little to no effects on veins
Hydralazine ADRs
Hypotension
Headache
Palpitations
GI disturbances
Facial flushing (rare)
Hydralazine dental
ortho hypo
direct renin inhibitor name/ form
Aliskerin (Tekturna)
Available: PO
Aliskerin moa
Decreases plasma renin activity
and inhibits the conversion of
angiotensinogen to angiotensin I
aliskerin adrs
Diarrhea, dyspepsia, hypotension
aliskerin dental
ortho hypo
ACEi names?
all end in -pril
Angiotensin receptor blockers (ARBs) names
all end in -sartan
ARBs moa
Blocks the AT1 receptor of
angiotensin II, preventing
vasoconstriction and
aldosterone secretion
ARBs adrs
do not cause what adrs?
Orthostatic hypotension
Headache
Dizziness
Hyperkalemia
Should not cause cough or angioedema
ARBs dental
ortho hypo
Angiotensin Receptor Neprilsyn Inhibitor (ARNI) name/ form
Sacubitril/Valsartan
(Entresto)
Available: PO
Sacubitril/Valsartan MOA
Sacubitril: inhibits neprilysin resulting in elevated levels
of B-type natriuretic peptide (BNP)
Valsartan: blocks the angiotensin II AT1 receptor
of angiotensin II
Sacubitril/Valsartan ADRs
Hypotension
Hyperkalemia
Angioedema (more than ACE inhibitors)
Sacubitril/Valsartan dental
hypo
Aldosterone antagonists names/forms
Eplerenone (Inspra) Available: PO
Spironolactone (Aldactone) Available: PO
aldo antag moa
Competitively inhibits the action of aldosterone at
mineralocorticoid receptors. Reducing blood pressure in a dose-dependent manner and preventing myocardial and vascula fibrosis
aldo antag ADRs
Hyperkalemia (16%)
Renal insufficiency
Gynecomastia (9% of males- spironolactone)
Dry mouth (rare
aldo antag dental
Monitor of dry mouth due
to diuretic effect
Dihydropyridine Rx’s
all end in -pine
Amlodipine (Norvasc) MOA
Inhibits calcium ions influx through L-type or “slow”
calcium channels”
Selective for vascular smooth muscle
same as all -pine Rx
amlodipine ADRs
Reflex tachycardia, flushing, hypotension, peripheral edema, gingival hyperplasia
Dihydropyridine Rx’s dental implications
Monitor of gingival
hyperplasia, usually
resolves upon
discontinuation
Clevidipine
(Cleviprex)
Only available as?
IV form
clevidipine MOA
Inhibits calcium ions influx
through L-type or “slow”
calcium channels”
Selective for vascular smooth
muscle
clevidipine ADrs
Reflex tachycardia,
flushing,
hypotension,
peripheral edema
Gingival hyperplasia not reported probably due to shorter duration of administration
felidipine MOA
Inhibits calcium ions influx
through L-type or “slow”
calcium channels”
Selective for vascular smooth
muscle
felodipine ADRs
Reflex tachycardia,
flushing,
hypotension,
peripheral edema,
gingival hyperplasia
Isradipine
(DynaCirc CR) MOA
Inhibits calcium ions influx
through L-type or “slow”
calcium channels”
Selective for vascular smooth
muscle
isradipine ADRs
Reflex tachycardia,
flushing,
hypotension,
peripheral edema
Information is sparse as to whether isradipine causes
gingival hyperplasia
Nicardipine
(Cardene)
Available in?
PO and IV
formulations
nicardipine MOA
Inhibits calcium ions influx
through L-type or “slow”
calcium channels”
Selective for vascular smooth
muscle
nicardipine ADRs
Reflex tachycardia,
flushing,
hypotension,
peripheral edema,
gingival hyperplasia
nicardipine dental implications
Xerostomia (normal salivary flow resumes upon discontinuation)
Monitor of gingival hyperplasia, usually resolves upon discontinuation
Nifedipine MOA
Inhibits calcium ions influx
through L-type or “slow”
calcium channels”
Selective for vascular smooth
muscle
nifedipine ADRs
Reflex tachycardia,
flushing,
hypotension,
peripheral edema,
gingival hyperplasi
nifedipine ADR
Gingival hyperplasia (10%
incidence with doses of
30-100mg/day). Effects
present after 1-9 months
of treatment. Usually
resolves upon
discontinuation
nimodipine MOA
Inhibits calcium ions influx
through L-type or “slow”
calcium channels”
Selective for vascular smooth
muscle
nimodipine ADR
Reflex tachycardia,
flushing,
hypotension,
peripheral edema
No reports of gingival hyperplasia with nimodipine
nimodipine dental implications
Possibly gingival
hyperplasia- although no
known cases
nisoldipine MOA
nhibits calcium ions influx
through L-type or “slow”
calcium channels”
Selective for vascular smooth
muscle
nisoldipine ADRs
Reflex tachycardia,
flushing,
hypotension,
peripheral edema
Information is sparse as to whether nisoldipine causes
gingival hyperplasi
nisoldipine dental
Xerostomia (normal salivary flow resumes upon discontinuation)
Possibly gingival hyperplasia- information is sparse
Non-Dihydropyridine Rx
selective for myocardium
Diltiazem and vermapril
Diltiazem MOA
inhibits calcium ions influx through L-type or “slow” calcium channels”
Selective for myocardial calcium channels
Slows impulse conduction through the AV node
diltiazem ADRs
Constipation,
dizziness,
lightheadedness,
hypotension,
bradycardia,
gingival hyperplasia
diltiazem dental
gingival hyperplasia
usually resolves
upon discontinuation
Verapamil MOA
where are impulses slowed in the cardiac conduction?
inhibits calcium ions influx through L-type or “slow”
calcium channels”
Selective for myocardial calcium channels
Slows impulse conduction through the AV node
verapamil ADRs
Constipation,
dizziness,
lightheadedness,
hypotension,
bradycardia,
gingival hyperplasia
verapamil dental
gingival hyper