Anti-hypertensive drugs
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Transcript of Anti-hypertensive drugs
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INTRODUCTION OF DRUG-DRUG INTERACTION OF ANTIHYPERTENSIVE
A drug interaction is a situation in which a substance (usually another
drug) affects the activity of a drug when both are administered
together.
Important drug-drug interaction of antihypertensive agent can be
caused by sharing of metabolic pathways with other drugs, either
inducing or inhibiting the metabolism. Most of effects are through
hepatic cytochrome p450. E.g. CYP3A is responsible for 40-60% of
traditional type hepatic drug-drug interaction.
The chance of drug-drug interaction increases, as increase in age
because elderly patient receive large number of drugs, and also due to
impaired renal excretion of some therapeutic agents as a result of
kidney impaired.
All beta blocker interfere with digitalis preparations and NSAIDs.
Orthostatic hypotension with beta blocker can be exacerbated by
ethanol or CNS depressants. Catecholamine-depleting drugs and beta
blocker can lead to bradycardia and heart attack. The cardiac effect of
nondihydropyridine calcium antagonists and lidocaine can be
potentiated by beta blocker. The effect of propranolol are potentiated
by ethanol, antithyroid drugs, tricyclic antideprassants and monoamine
oxidase inhibitor. likewise propranolol increase the effect of other
drugs e.g lidocaine, diazepam warfarin, theophylin, rizatriptan.
ACE inhibitor and angiotensin receptor blocker, these two classes of
antihypertensive drugs share their pathway to be adversely affected by
NSAIDs. Both classes of drug increase the risk of lithium toxicity and
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hyperkalemia. Diuretics increase blood pressure lowering effects of
both ACEI and ARBs. Telmisartan has drug interaction with digoxin that
increases the concentration of digoxin.
When patient takes alpha1 blocker and phosphodiesterase 5 inhibitors
the BP: Lowering effect of alpha1 inhibitor is affected. Both tadalafil
and vardenafil are contraindicated when patient is taking alpha1
blocker. The combination of verapamil and alpha blocker produce more
orthostatic hypotension and dizziness than either drug given alone.
Alpha2 agonist’s effect is interfered by NSAID and MAOIs, effect is
hypotension and sedation. Hypotensive effect of alpha2 agonist is
antagonized/inhibited by tricyclic antidepressant. Methyl dopa can
potentiate digoxin and lithium toxicity and antagonize effect of oral
hypoglycemic agents.
Antihypertensive agents also interact with cough and cold medication.
Many cough and cold medication contains NSAIDs for pain relief. NSAID
may increase blood pressure. Cough and cold medicine also contain
decongestant. Decongestant make blood pressure worse in 2 ways
1 Decongestant may increase blood pressure and heart rate.
2 Decongestant may prevent antihypertensive drug to function
properly.
ACE inhibitor enhanced hypotensive effect when sodium nitroprusside
given with ACEI.
Adrenergic neuron blocker enhanced hypotensive effect when given
with sodium nitroprusside.
ACE inhibitor enhance hypotensive effect when given with hydralazine.
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DRUG-DRUG INTERACTION WITH MECHANISM
DRUG
DRUG INTERACT . WITH
MECHANISM
propranolol Multivitamin with minerals
Minerals may decrease the effect of propranolol
propranolol
Alcohol
Additive effect in lowering your BP.
Bisoprolol
Theophylline
Combination causes bisoprolol less effective and increase effect of theophylline. bisoprolol reduce the CYP450 hepatic metabolism.
Metoprolol
Diltiazem
Additive reduction in heart rate cardiac conduction, cardiac contractility may occur when calcium channel blocker specially verapamil and diltiazem used with beta blocker.
Bepridil
Ciprofloxacin
Quinolones may cause dose related prolongation of QT intervals in some pt. that may result in elevated risk of arrhythmias, ventricular tachycardia.
Verapamil
fentanyl
Coadministration with inhibitors of CYP450 3A4 may increase plasma concentration of fentanyl, increase concentration could increase
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ADRs that may be fatal
Furodemide
Amikacin
Combination may cause nephrotoxicity due to additive or synergistic effect.
Furosemide
Lithium
Combination increase serum concentration of lithium. And cause lithium toxicity
Buemetanide Neomycin Combination may increase oto/ nephrotoxicity due to additive or synergistic effect.
Spironolactone quinapril Combination increase risk of hyperkalemia.
Nitroprusside Avanafil Combination causes sever hypotension and myocardial ischemia.
Spironolactone
candesartan
Combination increase risk of hyperkalemia. Life threatening and fatal hyperkalemia can occur especially when combination given to person who have renal impairment , diabetes, old age and sever heart failure.
Hydrochlorthiazide
Sodium biphosphate
Combination effect renal function/perfusion
Aliskiren
captopril
Combination causes renal complication,hyperkalemia,hypotension
Triamterene valsartan Increase serum concentration of potassium
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Lisinopril
leflunomide
Induce hepatotoxicity may potentiate liver injury associated with leflunomide.
Amlodipine Rifampicin Using amlodipine with rifampicin can decrease the effect of amlodipine.
Felodipine
Itraconazole
Itraconazole increase plasma level of felodipine
Isradipine
Dolasetron
Cause prolongation of PR and QRS intervals. Cardiac arrest and ventricular arrhythmias
Nisoldipine
Mifepristone
Mifepristone significantly increase plasma concentration of nisoldipine
Eplerenone clarithromycin Increase plasma concentration of eplerenone
Clonidine
Desipramine
Potentially life threatening elevation in BP when tricyclic antidepressant given with clonidine, enhancement of pressor response by TCA.
Guanfacine
Tizanidine
Tizanidine has alpha2 adrenergic activity and may potentiate hypotensive effect of other alpha2 adrenergic agonist.
Azilsartan medoxomil
Zolpidem Azilsartan and zolpidem have additive effect in lowering BP
Olmesartan
Pregabalin
Pregabalin is associated with development of angioedema. And when administered with olmesartan may increase the risk of angioedema. Specific
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symptoms include swelling of face , mouth and neck
Prazosin
Grastek
Immunotherapy with timothy grass pollen allergen extract can sometimes cause severe, even potentially life threatening allergic rxn that require emergency treatment with epinephrine, and prazocin can interfere with body’s response to epinephrine and significantly reduce its effect.
Benazepril
Ibuprofen
NSAID induced inhibition of renal prostaglandin synthesis which results in unopposed pressor activity producing hypertension in addition NSAID can cause fluid retention which also effects BP
Captopril furosemide These combination have additive effect. Coadministration cause hypotension and hypovolemia.
Ethacrynic acid
dronedarone
Dronedarone may cause dose related prolongation of QT interval. Hypokalemia and hypomagnesemia are known risk factor for arrhythmia associated with QT prolongation.
Nicardipine
Rifampin
Nicardipine together with rifampin can decrease the effects of nicardipine
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INTERACTON FOUND IN PRESCRIPTION
CORSAFE- NAVIDAT
Corsafe contains active ingredient amlodipine besylate and navidat
contains ciprofloxacin. when these 2 drugs are given in combination then
ciprofloxacin will interact with amlodipine and will increase plasma
concentration of amlodipine. In 8 elderly hypertensive pt. administration of
a single 5 mg dose of amlodipine in combination with moderate CYP450
3A4 inhibitor (ciprofloxacin 180mg orally daily for 3 days) resulted in nearly
60% increase in amlodipine peak plasma concentration and systemic
exposure.
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NAVIDAT- SURBEX,Z
As we know navidat contains amlodipine which is calcium channel blocker.
And surbex contains vitamins and minerals. Using amlodipine together with
multivitamin with minerals can decrease effect of calcium channel blocker.’
RENITEC-COXLAN
Renitec contains enalapril (ACEI) and coxlan contains meloxicam (NSAID).
When these are given in combination then NSAID will decrease
antihypertensive effect of ACEI. NSAID also cause fluid retention which
also affects blood pressure.
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LASORIDE – COXLAN
Lasoride is combination of furosemide and amiloride. And coxlan contains
meloxicam. when these medication are given in combination cause
interaction, NSAID and diuretic may adversely affect renal function due to
NSAID inhibition of prostaglandin that help renal perfusion in dehydrated
state. Hypotensive effect of diuretic may decrease because inhibition of
prostaglandin and can cause pressor activity and consequently elevation in
BP
TASMI – EPHAROX
Tasmi contain telmisartan and epharox contain piroxicam.
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Combination may reduce kidney function particularly in elderly or volume
depleted individual.
TASMI – PANADOL
There was no interaction found between them.
CIPEX –ENALAPRIL
Cipex contain ciprofloxacin . There was no interaction found between
ciprofloxacin and enalapril.
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CORSAFE- kARDURA
Corsafe contains amlodipine and kardura contains doxazosin. Both
increase blood pressure lowering effect. So should be given with precation
and with low doses otherwise it may cause hypotension.
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30 BRAND NAMES OF ANTIHYPERTENSIVE WITH
INDICATION, FREQUENCY, DOSAGE, SIDE EFFECT
COZAR (LOSARTAN )
FREQUENCY:-
Initial dose : 50mg orally once a day
Maintenance dose: 25 to 100 mg orally per day in 1 or 2 divided
doses
6 year or older,
Initial dose: 0.7mg/kg orally once a day (upto 50mg total)
DOSAGE = tablet,Film coated
INDICATIONS:-
Treatment of hypertension
To reduce the risk of stroke in patient with hypertension and left
ventricular hypertrophy.
Treatment of diabetic nephropathy with elevated serum creatinine
and proteninuria (urinary albumin to Creatinine ratio 300mg/g or
greater) in patients with 2 type diabetes and a history of hypertension.
ADR’S
Dizziness
Dry Cough
Back pain
Cold symptoms such as stuffy nose, sneezing,sore throat
In rare cases, cozaar cn cause a condition that results in the
breakdown of Skeletal muscle tissue, leading to kidney failure.
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TEVETEN (eprosartan)
Frequency
Initial dose: 600mg orally once a day
Maintenance dose 400 to 800 mg orally per day in 1 or 2 divided
doses
DOSAGE.
400mg pink,non-scored ,oval tablets
600mg white ,non-scored ,capsule-shaped tablets.
INDICATIONS
Teveten is indicated for the treatment of hypertension,it may be used
alone or in combination with other antihypertensives such as
diurentics and calcium channel blockers.
ADR’S
Burning or painful urination or changes in urinary frequency.
Cough
Fever
Sore throat
Abdominal or stomach pain
Joint pain
Unusual tiredness
CARDURA (doxazosin)
FREQUENCY
FOR HYPERTENSION
Initial dose: 1mg orally once a day
Maintenance dose: 1 to 16 mg orally once a day.
For Prostatic Hyperplasia
Initial Dose : 1mg orally once a day.
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Maintenance dose: Immediate-release: 1 to8mg orally once a day
.Depending on patient’s Symptomatic response and tolerability,the
dose may be increased to 8mg(the maximum recommended
dose).
DOSAGE = Tablet
INDICATIONS
Cardura is used to treat hypertension (high blood pressure), or to
improve urination in men with benign prostatic hyperplasia(enlarges
prostate)
ADR”S
Dizziness or lightheadedness
Blurred vision
Confusion
Dizziness,faintness, or lightheadedness when getting up form a lying
or sitting position
Fainting(sudden)
MINIPRESS (PRAZOSIN HYDROCHLORIDE)
FREQYENCY
Initial dose: 1mg or three times a day
Dosage may be slowly increased to a total daily dose of 20 mg given
in divided doses. The therapeutic dosages most commonly employed
have ranged from 6mg daily given in divided doses
INDICATIONS
Minipress is indicated for the treatment of hypertension,to lower blood
pressure.Lowering blood pressure reduces the rosk of fatal and
nonfatal cardiovascular events,primarily strokes and myocardial
infarctions.
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ADR’S
Dizziness or lightheadedness,especially when hetting up from a lying
or sitting position
Fainting(Sudden)
Loss of bladder control
Pounding heartbeat
Swelling of the feet or lower legs
Dryness of the mouth
Nervousness
Unusual tiredness or weakness
EDARBI (azilsartan)
FREQUENCY
INITIAL DOSE : 80mg orally once a day.It may be appropriate to
initiate dosage at 40mg orally once daily for patients who are treated
with high doses of diuretics.
MAINTANCE DOSE : 80mg orally once a day
DOSAGE “TABLET”
INDICATIONS
Edrabi is used to treat high blood pressure.
ADR’S
Hives ,Diffuculty Breating,swelling of your face,lips,tongue,or throat
Swelling in your feet or ankles
Diarehea
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BENICAR HCT (olmesartan/hydrochlorothiazide)
FREQUENCY
The recommended starting dose of BENICAR HCT is 40/12.5mg
once a day to patients whose blood pressure is not adequateley
controlled with olmesartan monotherapy.Dose can be titrated upto
40/25mg if necessary.
DOSAGE “FILM COATED TABLET
INDICATION
Treating high blood pressure.
ADR’S
Difficult ,burning,or painful urination
Flushed, dryskin.
Frequent urge to urinate
Fruit-like breath odor
Increased hunge
DIOVAN HCT (hydrochlorothiazide and valsartan)
FREQUENCY
The usual starting dose is diovan HCT160/12.5 mg once daily.The
dosage can be increased after 1 to 2 weeks of therapy to a maximum
of one 320/25 tablet once daily
DOSAGE “Tablet, film coated”
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INDICATION
Hydrochlorothiazide and valsartan is combination medicine used to
treat high blood pressure (hypertension).
ADR’S
Common(1 to 10)% Headache,fatigue,dizziness
Rare(less than 0.1%). Veryigo tinnitus.
INSPRA (eplerenone)
Frequency
The recommended starting dose of INSRA is 50mg administered
once daily.Increase the dosage of INSPRA to 50mg twice daily.
DOSAGE “Film Coated tablet”
INDICATION
Eplerenone os used to treat congestive heart failure after a heart
attack. Eplerenone is used to treat high blood pressure.
ADR’S
Cough,diarrhea,flu-like symptoms,and fatigue ,excess of cholesterol
in the blood
Excess of triglycerides in the blood.
LOTENSIN (benazepril)
FREQUENCY
10mg orally once a day
Maintenance dose: 20 to 40mg/day orally as a single dose or in two
equally divided doses
Maximum dose: 80mg/day
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DOSAGE “tablet”
INDICATION
Lotensin is used to treat high blood pressure.
ADR’S
Chills
Cold sweats
Confusion
Fast, irregular,pounding,or racing heartbeat or pulse
Feeling of warmth
CAPOTEN (capropril)
FRIQUENCY
The initial dose is 25mg b.i.d or t.i.d . If satisfactory reduction of blood
pressure has not been achieved after one or two weeks ,the dose
may be increased to 50mg b.i.d or t.i.d
DOSAGE “tablet 12.5mg
INDICATION
Capoten is used to treat high blood pressure ,congestive heart
failure,kidney problems caused by diabetes,and to improve survival
after a heart attack
ADR’S
Chest pain
Cloudy urine
Fast ,pounding, or irregular heartbeat or pulse
Dilated neck veins
MONPRIL (fosinopril)
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FREQUENCY
Initial dose 10mg orally once a day alone or in combination with
diuretic.
Maintenance dose: 20 to 40 mg orally once a day.
DOSAGE “ORAL TABLET
INDICATION
Monopril is used to treat high blood pressure or Heart failure.
ADR”S
Blurred vision
Chest pain or discomfort
Chills
Cold sweats
Confusion
Fast, slow, irregular heartbeat.
ACCUPRIL (quinapril)
FREQUENCY
Initial dose 10 or 20mg orally once a day in patient not on
diuretics
Maintenance dose 20 to 80mg orally per day,administered as a
single dose or in two equally divided doses.
DOSAGE “ORAL TABLET”
INDICATION
Accupril is used to treat high blood pressure and heart failure.
ADR’S
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Abdominal or stomach pain
Blurred vision
Chest pain
Confusion
Diarrhea
Difficult or labored breathing
PRINIVIL (Lisinopril)
FREQUENCY
Initial dose 10mg orally once a day,5mg orally once a day
Maintenance dose 20 to 40 mg orally once a day
Maximum dose 80 mg orally once a day
DOSAGE” ORAL TABLET & ORAL SOLUTION
INDICATION
Prinivil is used to treat high blood pressure or congestive heart
failure. It is also used to improve survival after a heart attack.
ADR’S
Dizziness
Hypotension
Hyperkalemia
Increased blood urea nitrogen
Increased serum creatinine
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TRANDATE (labetalol HCL)
FREQUENCY
The recommended initial dosage is 100mg twice daily whether used
alone or added to a diuretic regimen.After 2 or 3 days,using standing
blood pressure as an indicator,dosage may be titrated in increments
of 100 mg b.i.d. every 2 or 3 days.The usual maintenance dosage of
labetalol HCL is between 200 and 400mg twice daily.
DOSAGE “TABLET
INDICATION
Treating high blood pressure.It may be used alone or in combination
with other medicines, such as diuretics.
ADR’S
Orthostatic Hypotension,tightness in chest
Wheezing
TENORMIN (atenolol)
FREQUENCY
50 mg given as one tablet a day either alon or added to diuretic
therapy.Dose can be increase upto 100mg
DOSAGE = “IV SOLUTION & ORAL TABLET”
INDICATION
Tenormin is used to treat angina (chest pain) & hypertension
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ADR’S
Cardic failure
Dizziness
Fatigue
Bradycardia
Cold extremities
KERLONE (betaxolol HCL)
FREQUENCY
The initial dose of kerlone in hypertension is ordinarily 10mg once
daily either alone or added to diuretic therapy.The full
antihypertensive effect is usually seen within 7 to 14 days.If the
desired response is not achieved the dose can be doubled after 7 to
14 days.
DOSAGE “TABLET”
INDICATION
Betaxolol is used to treat hypertension
ADR’S
Headache
Bradycardia chest pain or discomfort
Lightheadedness ,dizziness or fainting
ZEBETA (bisoprolol FUMARATE)
FREQUENCY
The usual startin dose is 5mg once daily.The dose may be increased
to 10mg and then,If necessary,to 20 mg once daily.
DOSAGE “FILM COATED TABLET”
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INDICATION
Zebeta is used to treat hypertension
ADR’S
Body aches
Chest pain
Chills
Cough
Difficult or labored breathing
LOPRESSOR (metoprolol tartrate)
FREQUENCY
Initial 100mg Dailly in single or divided doses.The effective dosage
range of Lopressor tablets is 100-450 mg per day.
DOSAGE “TABLET,INJECTION”
INDICATION
Treating high blood pressure,alone or with other medicines.long term
treatment of chest pain,and reducing the risk of death because of
heart problems in patients who have a heart attach.
ADR’S
Cardiac failure and hypotension
Blurred vision
Chest pain or discomfort
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BYSTOLIC (nebivolol)
FREQUENCY
Starting dose is 5mg once daily, with or without food
DOSAGE = ORAL TABLET
INDICATION
BYSTOLIC IS USED TO TREAT HYPERTENSION
ADR’S
Tingling of the hands or feet
Unusual tiredness or weekness
Unususal weight gain or loss
Wheezing
VASCOR (bepridi)
FREQUENCY
100mg twice daily
DOSAGE = Available as film-coated tablets for oral use
INDICATION
Bepridil is used to treat hypertension and to treat angina (chest pain).
ADR’S
Palpitations and edema have been reported in 1% to 2% of patients.
Exacerbation of congestive heart failure has been associated with the
use of bepridil in 1% of patients.
25
CARDIZEM (diltiazem)
FREQUENCY
Extended Release Tablets.
Initial dose 180 to 240mg orally once a day.increasing the dose as
needed
Maximum dose540 mg/day
DOSAGE
Oral capsule extended release,oral capsule extended release 12
hr,oral capsule extended release 24 he,oral tablet extended release
INDICATION
Cardizem is used to treat hypertension Cardizem is also used to treat
chronic
Stable angina (chest pain)and angina due to coronary artery spasm.
ADR’S
Hoarseness
Tender or swollen glands in the neck
Trouble swallowing
Voice changes
VERALAN PM (verapamil)
FREQUENCY
Oral 200 mg orally once a day at bedtime
Maximum dose 400 mg/day
DOSAGE Extended Release Capsule
INDICATION
Verapamil is used to treat hypertension,angina and certain heart
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rhytm disorders.
ADR’S
Sinus bradycardia
Severe hypotension
Pulmonary edema
LASIX (furosemide)
FREQUENCY
Oral for hypertension
Initial 20 to 80mg per dose
Maintenance dose
Increase in increments of 20 to 40 mg/dose every 6 to 8 hours toi
desired effect the usual interval in once or twince daily,with maximum
daily dose of 600mg,
DOSAGE = Injection ,oral solution,oral tablet
INDICATION
Lasix is used to treat fluid retention (edema) in people with
congestive heart failure,liver disease,or a kidney disorder such as
nephrotic syndrome.
Lasix is also used to treat high blood pressure.
ADR’S
Sores,ulcers,or white spots on the lips or in the mouth
Swollen or painful glads
Tightness in chest
Unusual bleeding or bruising
27
BUMEX (bumetanide)
FREQUENCY
The usual total daiy dosage of bumex is 0.5mg to 2 mg and in most
patients is given as a single dose .
DOSAGE TABLET
INDICATION
Bumetanide trears fluid retention in people with congestive heart
failure,liver disease,or a kidney disorder such as nephrotic
syndrome,hypertension
ADR’S
Hypokalemia
Hyperurucemia
AIDACTONE (spironolactone)
FREQUENCY
50 to 100 mg of ALDACTONE administered in either single or divided
doses is recommended
DOSAGE Film coated tablet
INDICATION
Aldosterone is a hormone produced by your adrenal glands to help
regulate the salt and water balance in your body .Idactone alsi treat
fluid retention (edena) in people with congestive heart Failer ,cirrhosis
of the liver,or a kidney disorder called nephrotic syndrome.
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ADR’S
Abdominal or stomach cramping,burning,or tendetness
Bleeding gums
Bloody or black ,tarry stools
Bloody urine
Breast pain
Chest pain
NITROPRESS (Nitroprusside)
FREQUENCY
Initial dose 0.3mcg/kg/min IBW administered by continuous IV
infusion.
Mantenance dose The dose may be titrated upward to a maximum of
mcg/kg/min IBW
DOSAGE = I v powder for injection .iv solution
INDICATION
Nitroprusside is used to treat congestive heart failure and lift-threating
high blood pressure (hypertension). Nitroprusside is also used to
keep blood pressure low during a surgery.
ADR’S
Hypotension
Cyanide toxicity
Thiocyanate toxicity
LOTENSIN HCT (hydrichlorothiazide and benazepril)
FREQUENCY
Dose once daily. The dosage may then be increased after 2 to 3
weejs as needed to help achieve blood pressure goals.The maximum
29
recommended dose is 20mg/25mg.
DOSAGE oral tablet
INDICATION
Hydrochlorothiazide and benazepril us a combination medicine used
to treat hypertension
ADR’S
Rapid breathing
Selzures
Sweating
Thirst
Trembling
Unusual tiredness or weakness
VALTURNA (aliskiren and valsartan)
FREQUENCY
The recommended initial once daily dose of valturna is
150/160mg.Titrate as needed to a maximum of 300/320 mg.
DOSAGE Oral tablet
INDICATION
Valturna is used to treat high blood pressure
ADR’S
Bladder Pain
Bloody or cloudy urine
Body aches or pain
Chills
Cough
30
Diarehea
Difficult,Burning.or Painful urination
TARKA (trandolapril and verapamil)
FREQUENCY
Tarka have explored only once a day doses 4/240mg
DOSAGE = Oral tablet extended release
INDICATION
Trandolapril and verapamil is a combination medicine used to treat
high blood pressure.
ADR”S
Bradtcardia, first degree atrioventricular block,and second degree
atrioventricular block.
REFRENCE
FROM RIMINGTON
FROM LIPPINCOTT 4TH
EDITION
https://www.ncbi.nlm.nih.gov/pubmed/9397294
http://onlinelibrary.wiley.com/doi/10.1111/j.1524-
6175.2006.05939.x/full
https://www.drugs.com/