Week 7 Hypertension and Dyslipidemia Flashcards
ACE-I Angiotensin Converting Enzyme Inhibitors Drugs/Treat/MOA
PRIL drugs
HTN; first line
1st line for HTN and CKD and HTN and DM w/ albuminuria (renal protection)
MOA: prevent conversion of A1 to A2 via inhibition of ACE-1 enzyme
Hydrolyzes bradykinin
Some: HRT Failure/ Myocardial Infarction/ Nephropahty
***Helps prevent cardiac remodeling
ACE-1 ADE
PRIL drugs
Increase bradykinin: Dry non productive cough in 10% of patients (switch to ARB)
Angioedema (d/t ^ bradykinin)
Black BOX: do not use in pregnancy; can cause injury to fetal kidneys
First dose hypotension/HyperKalemia/increase serum Creatinine >30% ^ concerned for acute kidney injury (AKI)
**Captopril: neutropenia
ACE-I Drug Drug
PRIL- Druges
Caution with other drugs that increase potassium: Potassium sparing diuretics, SGLT2 inhibitors, Sulfamethoxazole-trimethoprim (increased risk in sudden death; abx used to treat UTI)
Do not prescribe ACE-1/ DRI/ ARB/ ARNIs
ACE-1 and ARNI: wash out period 36 hrs; risk hyperkalemia and angioedema
ACE-1 Prescribing Considerations
PRIL-Drugs
EnalaPRILat is the only IV formulation
No not start ACE-1 if K+ is >5.5
D/C ACE-I if SCr increases 30% from baseline
Should use with CKD patients but still watch SCr
All RAAS Drugs (ACE-1/ ARB/
ADE and Drug Drug Interactions
BLACK BOX: Fetal kidney injury
First Dose Hypotension
Hyperkalemia
Increase Serum Creatinine (SCr) AKI > 30%
AVOID ACE-I/ ARB/ DRI/ ARNI
Potassium increasing drugs: Potassium-sparing diuretics/ SGLT2 inhibitors/ Sulfamethoxazole-trimethoprim
Triple Whammy: RAAS/ NSAID/ACE-I or ARB
Dehydration: AKI
Lithium: neurological and N/V Hypotension
Angiotensin II Receptor Blockers (ARB) Drugs/ Treat/ MOA
SARTAN Drugs
HTN 1st line therapy
Approved 1st line with HTN and CKD and HTN and DM w/ albuminuria
MOA: Angiotensin 1 receptor antagonist throughout the body which in turn blocks angiotensin II from binding– so it blockers II
Some: Heart Failure; Myocardial Infarction; Nephropathy
***Helps prevent cardiac remodeling
ARB ADE
SARTAN- Drugs
ADE: Dry cough but only in 3%
Angioedema but lower risk than ACE-I
Switching from ACE-I to ARB for dry cough or to prevent angioedema worth trying especially when preventing cardiac remodeling
Less risk of cough and hyperkalemia than ACE-I// higher risk of hypotensive episodes
Direct Renin Inhibitors (DRI)
Only 1 drug/ Drug/ Treat/ MOA
ADE/ DRUG DRUG
Aliskiren (REN for Renin)
Treat hypertension; not 1st line drug
^Risk cardiac events (rarely used in practice)
MOA: Decreases renin activity
SAME ADE and Drug drug as RAAS
Thiazide and Thiazide Like Diuretics
Drugs/ Treat/ MOA
Drugs:
Most used: ChlorTHALIdone and
IndapamIDE
OG: HydrchlororoTHIAZIDE
MetolAZone
Treat: hypertension (first line)
Edema
MOA: Inhibit NA and H2O reabsorption at the distal convoluted tubule so there fore keeps water be excreted
Excrete K and M (Hypokalemia)
**not a strong diuretic, preferred for HTN but not HRT failure; further down tubule so not as strong
Thiazide ADE
Same Drug Drug as RAAS
Drugs:
Most used: ChlorTHALIdone and
IndapamIDE
OG: HydrchlororoTHIAZIDE
MetolAZone
Dermatologic: sunburn and increased risk for squamous and basal cell carcinoma
Sulfa/ Sulfonamide allergy
Sexual Dysfunction: up to 25% of males (on ChlorTHALidone)
Hyper GLUC (Hydrochlorothiazide)
G=^ glucose (watch diabetes) L=^Lipids
U=^ Uric acid (watch gout)
C=^ Calcium (helpful for osteoporosis)
Chlorthalidone: ^risk hypokalemia (8%)
Indapamide: lowest risk hypokalemia and neutral glucose and lipids
Thiazide Prescribing Considerations
Drugs:
Most used: ChlorTHALIdone and
IndapamIDE
OG: HydrchlororoTHIAZIDE
MetolAZone
Always prescribe to take in the morning once daily to avoid nocturia
Chlorthaldone and Indapamide first choice for longer half life and greater effectiveness than hydrochlorothiazide
If CrCl<30 Thiazides will not work; except for Indapamide: approved to CrCl of 10
Use lowest dose possible; increase dose does not > effect but it does >ADE
Monitor Elytes around 2 weeks and 6-12 months after
Potassium Sparing Diuretics
Drugs/ Treat/ Use/ MOA
Triamterene and Amiloride
Treat: Edema (very weak)
Add to Thiazide to counter hypokalemia; no ordered individually for HTN
Common: Hydrochlorothiazide/triamterene
MOA: late distal convoluted tubule and collecting duct
Same Drug Drug as RAAS and Thiazide
RISK HYPERKALEMIA: check levels and do not give with ACE-I/ARB/REN
But give with Thiazide to prevent hypokalemia
Dihydropyridine (DHP) Calcium Channel Blockers (CCB)
Drugs/ Treat/ MOA
CCB: DIPINE Drugs
HTN First line drug
DHP treat D’ High Pressure
Also: Stable angina/ migraine/ anal fissure
**Nifedipine: pregnancy HTN and tocolytic
**Nimodipine: Subarachnoid Hemorrhage
MOA: act on calcium channels in smooth vascular muscles of arterioles
CCB ADE
DIPINE-Drugs
Only enteral; IV known to cause death
Hypotension with reflex tachycardia (Barro receptors) This is why only use with stable angina; rebound tachy can cause MI
Dose dependent peripheral edema
***NOT fluid retention NO DIURETIC; use and ACE-I or ARB
CCB: arterial vasodilation
ACE-I/ARB: venodilation
AldosterONE Antagonists
Drugs/ Treat/ MOA
SpironolacTONE and EplereNONE
OG: Non selective SpironolacTONE: HTN, HRT failure, ascites, acne vulgars, hirsutism; therapy transgender feminizing hormone
EplereNONE: HTN and HRT failure
MOA: Both block the action of aldosterone in the distal nephron
Spironolactone also blocks androgen
AldosterONE Antagonists
SpironolacTONE and EplereNONE
Hyperkalemia
Spironolactone: Anti Androgen Effects: gynecomastia/ impotence/ Menstrual irregularities
Monitor with other drugs that can cause hyperkalemia
Beta Blockers
1st Gen
2nd Gen
3rd Gen
OLOL-Drugs
1st Gen: Beta 1/2 blockers: start with N-Z
2nd Gen: Beta 1 blockers: start with A-M
3rd Gen: Beta Blocker and vasodilatory mechanisms (carvedilol, labetalol, nebivolol)
Non Selective Beta Blockers: First Generation
ADE
OLOL Drugs N-Z
Treat: HTN/ HRT failure/ Angina/ AFib/ Migraine/ Tremor/
Propranolol (for PROfessionals): performance anxiety
Timolol: glaucoma eye drops
Blockade of Beta 1 and Beta 2
***Sotalol also blocks potassium channels (class 3 antidysrhythmic)
BOX Warning: Ischemic HRT disease with abrupt d/c (restart ASAP post operative)
Bradyarrhythmias (bradycardia and AV Blocks)
Bronchospasm: NOT for COPD/ Asthma
CNS Effects: fatigue/ sexual disorders/ depression
Hypoglycemia masking: be careful with diabetes
Selective Beta Blocker: Second Generation
OLOL-Drugs A-M
Treat HTN/ HRT Failure, angina, AFib, migraine
Used with HTN with present cardiac condition
MOA: selective Beta 1 receptor found on the heart
BOX Warning: Ischemic HRT disease with abrupt d/c (restart ASAP post operative)
Bradyarrhythmias (bradycardia and AV Blocks)
Bronchospasm: MUCH LESS
CNS Effects: fatigue/ sexual disorders/ depression
Hypoglycemia masking: be careful with diabetes
Metoprolol tartate (Lopressor): immediate release 2-4 times daily
Metoporol succinate (Toprol XL): long acting extended release once daily– think SUX= XL
Beta Blocker Third Generation
Carvedilol/ Labetalol/ Nebivolol
Treat: HTN/ HRT Failure/ Angina/ Afib/ mirage
Carvedilol: CAR=Cardiac; FDA approved for HRT Failure
Labetalol: Lab=Labor; pregnancy
Nebivolol: N= iNO; release iNO reducing systemic vascular resistance
BOX Warning: Ischemic HRT disease with abrupt d/c (restart ASAP post operative)
Bradyarrhythmias (bradycardia and AV Blocks)
Bronchospasm: C/I in ASTHMA and COPD
CNS Effects: fatigue/ sexual disorders/ depression
Hypoglycemia masking: be careful with diabetes
Alpha Blockers
Drugs/ Treat/ MOA
SIN-Drugs
Conventional: (ZOSIN)
PraZOSIN
DoxaZOSIN
TeraZOSIN
Urologic/Selective: Alpha 1A benign prostatic hyperplasia and kidney stones
(ALL OSIN)
ALfuzOSIN
SilodOSIN (Flomax)
TamsulOSIN (Rapaflo)
MOA: alpha 1 receptors (1A 1B 1D)
ADE:
First dose phenomenon: profound orthostatic hypertension; falls risk; take at bedtime (BEERS list)
Floppy Iris Syndrome: Alpha 1 undergoing cataract surgery
Sexual Dysfunction (EJ decreased)
Alpha 2 Agonists
Drugs/ Treat/ MOA/ ADE
Clonidine/ Methyldopa (pregnancy)/ Guafacine (ADHD)
Treat: withdrawal/ substance use disorder/ vasomotor symptoms with menopause/ HTN/ ADHD
MOA: Alpha 2 presynaptic receptors within brainstem: A2 Agonist will cause a negative feedback loop to shut down sympathetic nervous system < HR < BP < Adrenyline– can cause withdrawal symptoms is stopped suddenly
ADE: Epidural use for pain only when monitored
Bradycardia/ hypotension
Sedation and dry mouth
Withdrawal symptoms (wean slowly)
Direct Vasodilators
Drugs/ Uses/ MOA
Hydralazine, Minoxidil
Hydralazine: Emergent HTN; Emergent HTN in pregnancy; Hrt failure
Minoxidil: HTN; topical for alopecia
MOA: Directly relax smooth muscle with little effort on veins
Direct Vasodilators
ADE
Minoxidil Box Warning: Pericardial effusion; only use in pts who have not responded to a diuretic and two other antihypertensive agents
Box Warning II: uses with a Beta Blocker to prevent tachycardia and increased myocardial workload
Hydralazine: Induce lupus like syndrome
Hypotension with reflex tachycardia
Long term use can cause Na + H2O retention: use with a diuretic
Hypertension Pregnancy Drugs
NIfedipine (1st line)
Labetalol
Methyldopa
Hydralazine
Thiazide diuretics
“Hot Mamas Need Love”
Hydralazine (HTN emergency)
Methydopa (a2 agonist)
Nifedipine (DHP-CCB 1st line)
Labetolol (non selective B-Blocker)
AVOID RAAS: Kidney damage to fetus
Initial HTN Drug Selection
First Line Drugs
ACE-1/ ARB
DHP CCB
Thiazide/Thiazide-Like diuretic
***Most important thing is BP reduction not initial drug selection
Start low, go slow
If BP not controlled with initial dose then increase once; if still not enough then add an additional drug (better to add a drug than go up to avoid worse ADE)
***BP is more than 20/10mmHg above goal; combo therapy should be initiated first
Drug Hierarchy HTN
First Line:
ACE-1/ ARB
DHP CCB
Thiazide/ like drug
Second Line: use a combo of above
Third Line: Use a combo of above plus a Thiazide diuretic
Fourth Line: Aldosterone Antagonist
Fifth Line: Beta Blocker: Carvedilol, Lebetaol, Nebivolol
Sixth Line: Any other classes
Co-morbidities with HTN FIRST LINE:
MI/HF/Angina: beta blocker
CKD: ACE-I/ ARB
DM w/ albuminuria: ACE-I/ ARB
HTN Monitoring when Treating
B/P every 4 weeks till at goal
Q 2 weeks for severely high BP
Once at goal reassess every 3-6 months
Labs (Elytes and SCr)
reassess 1-3 post initiation/ titration
Then annually
HTN Emergency
Nitrates
: vascular smooth muscle relaxation
Sodium Nitroprusside:
BOX WARNING: Hypotension and ischemia; Must reconstitute
Nitrates: BOX WARNING: Cyanide toxicity; caution with renal impairment in older adults
HMG-CoA Reductase Inhibitors
Hydrophilic vs Lipophilic
CYP3A4 metabolism vs other routes
High Intensity Therapy choice
STATIN- Drugs
Hydrophilic: rosuvastatin, pravastatin
Lipophilic: all others
CYPO3A4 metabolism: Atorvastatin, Lovastatin, Simvastatin
High Intensity: Atorvastatin (40-80), rosuvastatin (20-40)
HMG-CoA Reductase Inhibitors
Uses/ MOA
STATINS
hypercholesterolemia
Primary and secondary (prevent subsequent events) prevention of CV events
First choice CV reduction in: diabetes and post MI
MOA: Inhibit HMG-CoA Reductase, a rate limiting step of cholesterol synthesis in the liver : trying to catch and pull cholesterol from the blood stream
Pleiotropic Benefit: can lower CRP
Effects LDL, TG, HDL
STATIN HMG-CoA
ADE
ADE:
Myopathy (muscle pain) and Rhabdomyolysis (rapid muscle break down)
5-10% pts myopathy: will resolve is medication is stopped
check CK (creatine kinase)
Try hydrophilic statin; may not move as easily into muscle cells
Diabetes Warning: 1/500 pts at risk for developing diabetes; CV benefit outweighs risk
Memory impairment? BBB crossing; Not proven
Hepatoxicity: Baseline LFT and then as needed
STATIN HMG-CoA
Drug Drug
check CK levels when used with Daptomycin (strong ABX)
W/ Fibrates may increase myopathy
CYP3A4 Statins (PACMAN loves Grapefruit juice
STATIN HMG-CoA
Prescribing Considerations
Rosuvastatin: pts of East Asian descent were found to have two-fold higher levels
Do not use in pregnancy or breastfeeding
Therapy is lifelong
High Intensity drugs do not mean Higher risk for ADE
Admin at bedtime (you create cholesterol primarily at night
Simvastatin only 20mg with amlodipine
Lipid panel baseline and then every 4-6 weeks after initiation/titration and then every 3-12 months
Who gets a STATIN
Primary Prevention:
age 30-79yrs
LDL >190= high intensity statin
LDL= 70-190
Diabetes: moderate intensity unless ASCVD risk then high intensity
No Diabetes: 10 yr ASCVD risk calculator
<5% life style
5-7.5% moderate and lifestyle
7.5-20% moderate
>20% high intensity
Cholesterol Absorption Inhibitors
Drug/ USE/ MOA
Ezetimibe
Alternative to STATIN (myopathy)
Benefit if uses with STATIN
MOA: inhibits absorption at the brush border of the small intestine
Reduces cholesterol in liver
Effect on LDL, TG, HDL
Cholesterol Absorption Inhibitor
ADE and considerations
Ezetimibe
Myopathy; rare hepatotoxicity; do not use in pregnancy or breastfeeding
Simvastatin and Ezetimibe: combo therapy great CV reduction
PCSK-9 Inhibitors
Monoclonal antibodies
Drugs/ Uses/ MOA/ ADE
Evolocumab
Alirocumab
MABs (monoclonal antibodies)
Familiar and primary hypercholesterolemia
MOA: monoclonal antibody binds to and inhibits PCSK-9; results in more LDL receptors and reduced LDL
ADE: Inject site reactions
one of the newest drugs on the market; expensive and long term data unknown
Fibrates
Drugs/ Use/ MOA
FenoFIBRATE
GemFIBRozil
FenoFIBRic Acid
Treat hypertriglyceridemia
^TG
MOA: PPAR- alpha agonist, resulting in lower TG levels
ADE: myopathy (esp when combined with other drugs)
Hepatoxicity
Gall stones; CONTRAINDICATED in GALL BLADDER DISEASE)
Drug Drug: GemFIBRolzil can cause bleeding risk in pts on warfarin
Bile Acid Sequestrants
Drug/ Uses/ MOA/ ADE
CHOLESevelam
CHOLEStyramine
COLEStipol
Use: dyslipidemia adjunct; diarrhea with bile acid malabsorption; diabetes adjunct (cholesevelam); hyperthyroidism (cholestyramine specific)
MOA: resin binds to bile acid preventing their absorption and promoting excretion
GI: constipation, cramping, bloating
Malabsorption of fat soluble vitamins (ADEK)
Malabsorption of other drugs (separate by 2-4 hour window)
Gallstones
Colesvelam preferred d/t lowest ADE
CONTRAINDICATED: DO NOT GIVE if TG>300 (can increase) and with gallbladder disease
