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Tablets, USP · STAT Rx USA LLC
Dosage Form
Tablets, USP
Manufacturer
STAT Rx USA LLC
This medication contains important usage instructions, warnings, and side effect information that you should review before use.
USE IN PREGNANCY
, When pregnancy is detected, losartan potassium tablets should be discontinued as soon as possible. See . When used in pregnancy during the second and third trimesters drugs that act directly on the renin-angiotensin system can cause injury and even death to the developing fetus. WARNINGS, Fetal/Neonatal Morbidity and Mortality
Hypertension
Losartan potassium tablets are indicated for the treatment of hypertension. It may be used alone or in combination with other antihypertensive agents, including diuretics.
Hypertensive Patients with Left Ventricular Hypertrophy
Losartan potassium tablets are indicated to reduce the risk of stroke in patients with hypertension and left ventricular hypertrophy, but there is evidence that this benefit does not apply to Black patients. (See and , PRECAUTIONS Race , CLINICAL PHARMACOLOGY , , .) Pharmacodynamics and Clinical Effects Reduction in the Risk of Stroke Race
in 2 Patients Nephropathy Type Diabetic
Losartan potassium tablets are indicated for the treatment of diabetic nephropathy with an elevated serum creatinine and proteinuria (urinary albumin to creatinine ratio ≥300 mg/g) in patients with type 2 diabetes and a history of hypertension. In this population, losartan potassium tablets reduce the rate of progression of nephropathy as measured by the occurrence of doubling of serum creatinine or end stage renal disease (need for dialysis or renal transplantation) (see , CLINICAL PHARMACOLOGY ). Pharmacodynamics and Clinical Effects
Adult Hypertensive Patients
Losartan potassium tablets may be administered with other antihypertensive agents, and with or without food.
Dosing must be individualized. The usual starting dose of losartan potassium tablets is 50 mg once daily, with 25 mg used in patients with possible depletion of intravascular volume ( patients treated with diuretics) (see and patients with a history of hepatic impairment (see Losartan potassium tablets can be administered once or twice daily with total daily doses ranging from 25 mg to 100 mg. e.g., , WARNINGS ) Hypotension ─ Volume-Depleted Patients , PRECAUTIONS ). General
If the antihypertensive effect measured at trough using once-a-day dosing is inadequate, a twice-a-day regimen at the same total daily dose or an increase in dose may give a more satisfactory response. The effect of losartan is substantially present within one week but in some studies the maximal effect occurred in 3-6 weeks (see Hypertension). , CLINICAL PHARMACOLOGY , Pharmacodynamics and Clinical Effects
If blood pressure is not controlled by losartan potassium tablets alone, a low dose of a diuretic may be added. Hydrochlorothiazide has been shown to have an additive effect (see Hypertension). , CLINICAL PHARMACOLOGY , Pharmacodynamics and Clinical Effects
No initial dosage adjustment is necessary for elderly patients or for patients with renal impairment, including patients on dialysis.
Pediatric Hypertensive Patients ≥6 years of age
The usual recommended starting dose is 0.7 mg/kg once daily (up to 50 mg total) administered as a tablet or a suspension (see ). Dosage should be adjusted according to blood pressure response. Doses above 1.4 mg/kg (or in excess of 100 mg) daily have not been studied in pediatric patients (See and and Preparation of Suspension , CLINICAL PHARMACOLOGY , Pharmacokinetics Special Populations , Pharmacodynamics and Clinical Effects , WARNINGS .). Hypotension ─ Volume-Depleted Patients
Losartan potassium tablets are not recommended in pediatric patients <6 years of age or in pediatric patients with glomerular filtration rate <30 mL/min/1.73 m (see and 2 , CLINICAL PHARMACOLOGY , , , Pharmacokinetics Special Populations Pharmacodynamics and Clinical Effects ). PRECAUTIONS
Preparation of Suspension (for 200 mL of a 2.5 mg/mL suspension)
Add 10 mL of Purified Water USP to an 8 ounce (240 mL) amber polyethylene terephthalate (PET) bottle containing ten 50 mg losartan potassium tablets. Immediately shake for at least 2 minutes. Let the concentrate stand for 1 hour and then shake for 1 minute to disperse the tablet contents. Separately prepare a 50/50 volumetric mixture of Ora-Plus and Ora-Sweet SF . Add 190 mL of the 50/50 Ora-Plus /Ora-Sweet SF mixture to the tablet and water slurry in the PET bottle and shake for 1 minute to disperse the ingredients. The suspension should be refrigerated at 2-8°C (36-46°F) and can be stored for up to 4 weeks. Shake the suspension prior to each use and return promptly to the refrigerator. TM** TM** TM TM
**Trademark of Paddock Laboratories, Inc.
Hypertensive Patients with Left Ventricular Hypertrophy
The usual starting dose is 50 mg of losartan potassium tablets once daily. Hydrochlorothiazide 12.5 mg daily should be added and/or the dose of losartan potassium tablets should be increased to 100 mg once daily followed by an increase in hydrochlorothiazide to 25 mg once daily based on blood pressure response (see , CLINICAL PHARMACOLOGY , ). Pharmacodynamics and Clinical Effects Reduction in the Risk of Stroke
in 2 Patients Nephropathy Type Diabetic
The usual starting dose is 50 mg once daily. The dose should be increased to 100 mg once daily based on blood pressure response (see in 2 Patients). Losartan potassium tablets may be administered with insulin and other commonly used hypoglycemic agents ( . ., sulfonylureas, glitazones and glucosidase inhibitors). , CLINICAL PHARMACOLOGY , Nephropathy Pharmacodynamics and Clinical Effects Type Diabetic e g
Losartan potassium tablets are contraindicated in patients who are hypersensitive to any component of this product.
Hypertension
Losartan potassium tablets have been evaluated for safety in more than 3300 adult patients treated for essential hypertension and 4058 patients/subjects overall. Over 1200 patients were treated for over 6 months and more than 800 for over one year. In general, treatment with losartan potassium tablets were well-tolerated. The overall incidence of adverse experiences reported with losartan potassium tablets were similar to placebo.
In controlled clinical trials, discontinuation of therapy due to clinical adverse experiences was required in 2.3 percent of patients treated with losartan potassium tablets and 3.7 percent of patients given placebo.
The following table of adverse events is based on four 6- to 12-week, placebo-controlled trials involving over 1000 patients on various doses (10-150 mg) of losartan and over 300 patients given placebo. All doses of losartan are grouped because none of the adverse events appeared to have a dose-related frequency. The adverse experiences reported in ≥1% of patients treated with losartan potassium tablets and more commonly than placebo are shown in the table below.
|
|
Losartan
|
Placebo
|
|
|
(n=1075)
|
(n=334)
|
|
|
Incidence %
|
Incidence %
|
|
Musculoskeletal
|
|
|
| Cramp, muscle
|
1
|
0
|
| Pain, back
|
2
|
1
|
| Pain, leg
|
1
|
0
|
|
|
|
|
|
Nervous
System
/
Psychiatric
|
|
|
| Dizziness
|
3
|
2
|
|
|
|
|
|
Respiratory
|
|
|
| Congestion, nasal
|
2
|
1
|
| Infection, upper respiratory
|
8
|
7
|
| Sinusitis
|
1
|
0
|
The following adverse events were also reported at a rate of 1% or greater in patients treated with losartan, but were as, or more frequent, in the placebo group: asthenia/fatigue, edema/swelling, abdominal pain, chest pain, nausea, headache, pharyngitis, diarrhea, dyspepsia, myalgia, insomnia, cough, sinus disorder.
Adverse events occurred at about the same rates in men and women, older and younger patients, and Black and non-Black patients.
A patient with known hypersensitivity to aspirin and penicillin, when treated with losartan potassium tablets, was withdrawn from study due to swelling of the lips and eyelids and facial rash, reported as angioedema, which returned to normal 5 days after therapy was discontinued.
Superficial peeling of palms and hemolysis were reported in one subject.
In addition to the adverse events above, potentially important events that occurred in at least two patients/subjects exposed to losartan or other adverse events that occurred in <1% of patients in clinical studies are listed below. It cannot be determined whether these events were causally related to losartan:
facial edema, fever, orthostatic effects, syncope; Body as a Whole:
angina pectoris, second degree AV block, CVA, hypotension, myocardial infarction, arrhythmias including atrial fibrillation, palpitation, sinus bradycardia, tachycardia, ventricular tachycardia, ventricular fibrillation; Cardiovascular:
anorexia, constipation, dental pain, dry mouth, flatulence, gastritis, vomiting; Digestive:
anemia; Hematologic:
gout; Metabolic:
arm pain, hip pain, joint swelling, knee pain, musculoskeletal pain, shoulder pain, stiffness, arthralgia, arthritis, fibromyalgia, muscle weakness; Musculoskeletal:
anxiety, anxiety disorder, ataxia, confusion, depression, dream abnormality, hypesthesia, decreased libido, memory impairment, migraine, nervousness, paresthesia, peripheral neuropathy, panic disorder, sleep disorder, somnolence, tremor, vertigo; Nervous System/Psychiatric:
dyspnea, bronchitis, pharyngeal discomfort, epistaxis, rhinitis, respiratory congestion; Respiratory:
alopecia, dermatitis, dry skin, ecchymosis, erythema, flushing, photosensitivity, pruritus, rash, sweating, urticaria; Skin:
blurred vision, burning/stinging in the eye, conjunctivitis, taste perversion, tinnitus, decrease in visual acuity; Special Senses:
impotence, nocturia, urinary frequency, urinary tract infection. Urogenital:
Persistent dry cough (with an incidence of a few percent) has been associated with ACE-inhibitor use and in practice can be a cause of discontinuation of ACE-inhibitor therapy. Two prospective, parallel-group, double-blind, randomized, controlled trials were conducted to assess the effects of losartan on the incidence of cough in hypertensive patients who had experienced cough while receiving ACE-inhibitor therapy. Patients who had typical ACE-inhibitor cough when challenged with lisinopril, whose cough disappeared on placebo, were randomized to losartan 50 mg, lisinopril 20 mg, or either placebo (one study, n=97) or 25 mg hydrochlorothiazide (n=135). The double-blind treatment period lasted up to 8 weeks. The incidence of cough is shown below.
Study 1 HCTZ Losartan Lisinopril †
________________________________________________________________________
Cough 25% 17% 69%
Study 2 Placebo Losartan Lisinopril ††
________________________________________________________________________
Cough 35% 29% 62%
Demographics = (89% caucasian, 64% female) †
Demographics = (90% caucasian, 51% female) ††
These studies demonstrate that the incidence of cough associated with losartan therapy, in a population that all had cough associated with ACE-inhibitor therapy, is similar to that associated with hydrochlorothiazide or placebo therapy.
Cases of cough, including positive re-challenges, have been reported with the use of losartan in post-marketing experience.
No relevant differences between the adverse experience profile for pediatric patients and that previously reported for adult patients were identified. Pediatric Patients:
Patients Left Hypertrophy Hypertensive with Ventricular
In the LIFE study, adverse events with losartan potassium tablets were similar to those reported previously for patients with hypertension.
in 2 Patients Nephropathy Type Diabetic
In the RENAAL study involving 1513 patients treated with losartan potassium tablets or placebo, the overall incidences of reported adverse experiences were similar for the two groups. Losartan potassium tablets were generally well tolerated as evidenced by a similar incidence of discontinuations due to side effects compared to placebo (19% for losartan potassium tablets, 24% for placebo). The adverse experiences, regardless of drug relationship, reported with an incidence of ≥4% of patients treated with losartan potassium tablets and occurring more commonly than placebo, on a background of conventional antihypertensive therapy, are shown in the table below.
|
|
Losartan and Conventional Antihypertensive Therapy Incidence % (n=751)
|
Placebo and Conventional Antihypertensive Therapy Incidence % (n=762)
|
|
Body
as
a
Whole
|
|
|
| Asthenia/Fatigue
|
14
|
10
|
| Chest Pain
|
12
|
8
|
| Fever
|
4
|
3
|
| Infection
|
5
|
4
|
| Influenza-like disease
|
10
|
9
|
| Trauma
|
4
|
3
|
|
Cardiovascular
|
|
|
| Hypotension
|
7
|
3
|
| Orthostatic hypotension
|
4
|
1
|
|
Digestive
|
|
|
| Diarrhea
|
15
|
10
|
| Dyspepsia
|
4
|
3
|
| Gastritis
|
5
|
4
|
|
Endocrine
|
|
|
| Diabetic neuropathy
|
4
|
3
|
| Diabetic vascular disease
|
10
|
9
|
|
Eyes
,
Ears
,
Nose
and
Throat
|
|
|
| Cataract
|
7
|
5
|
| Sinusitis
|
6
|
5
|
|
Hemic
|
|
|
| Anemia
|
14
|
11
|
|
Metabolic
and
Nutrition
|
|
|
| Hyperkalemia
|
7
|
3
|
| Hypoglycemia
|
14
|
10
|
| Weight gain
|
4
|
3
|
|
Musculoskeletal
|
|
|
| Back pain
|
12
|
10
|
| Leg pain
|
5
|
4
|
| Knee pain
|
5
|
4
|
| Muscular weakness
|
7
|
4
|
|
Nervous
System
|
|
|
| Hypesthesia
|
5
|
4
|
|
Respiratory
|
|
|
| Bronchitis
|
10
|
9
|
| Cough
|
11
|
10
|
|
Skin
|
|
|
| Cellulitis
|
7
|
6
|
|
Urogenital
|
|
|
| Urinary tract infection
|
16
|
13
|
Post-Marketing Experience
The following additional adverse reactions have been reported in post-marketing experience:
: Hepatitis (reported rarely). Digestive
Malaise. General Disorders and Administration Site Conditions:
: Thrombocytopenia (reported rarely). Hemic
: Angioedema, including swelling of the larynx and glottis, causing airway obstruction and/or swelling of the face, lips, pharynx, and/or tongue has been reported rarely in patients treated with losartan; some of these patients previously experienced angioedema with other drugs including ACE inhibitors. Vasculitis, including Henoch-Schonlein purpura, has been reported. Anaphylactic reactions have been reported. Hypersensitivity
Hyperkalemia, hyponatremia have been reported with losartan. Metabolic and Nutrition:
Rare cases of rhabdomyolysis have been reported in patients receiving angiotensin II receptor blockers. Musculoskeletal:
Dysgeusia Nervous system disorders:
Dry cough (see above). Respiratory:
Erythroderma Skin:
Laboratory Test Findings
In controlled clinical trials, clinically important changes in standard laboratory parameters were rarely associated with administration of losartan potassium tablets.
, Minor increases in blood urea nitrogen (BUN) or serum creatinine were observed in less than 0.1 percent of patients with essential hypertension treated with losartan potassium tablets alone (see ). Creatinine Blood Urea Nitrogen: , PRECAUTIONS Impaired Renal Function
Small decreases in hemoglobin and hematocrit (mean decreases of approximately 0.11 grams percent and 0.09 volume percent, respectively) occurred frequently in patients treated with losartan potassium tablets alone, but were rarely of clinical importance. No patients were discontinued due to anemia. Hemoglobin and Hematocrit:
Occasional elevations of liver enzymes and/or serum bilirubin have occurred. In patients with essential hypertension treated with losartan potassium tablets alone, one patient (<0.1%) was discontinued due to these laboratory adverse experiences. Liver Function Tests:
Significant lethality was observed in mice and rats after oral administration of 1000 mg/kg and 2000 mg/kg, respectively, about 44 and 170 times the maximum recommended human dose on a mg/m basis. 2
Limited data are available in regard to overdosage in humans. The most likely manifestation of overdosage would be hypotension and tachycardia; bradycardia could occur from parasympathetic (vagal) stimulation. If symptomatic hypotension should occur, supportive treatment should be instituted.
Neither losartan nor its active metabolite can be removed by hemodialysis.
Losartan potassium is an angiotensin II receptor (type AT ) antagonist. Losartan potassium, a non-peptide molecule, is chemically described as 2-butyl-4-chloro-1-[ -( - -tetrazol-5-ylphenyl)benzyl]imidazole-5-methanol monopotassium salt. 1 p o 1H
Its empirical formula is C H ClKN O, and its structural formula is: 22 22 6
[image: MM1]Losartan potassium, USP is a white to off-white free-flowing crystalline powder with a molecular weight of 461.01. It is freely soluble in water, soluble in alcohols, and slightly soluble in common organic solvents, such as acetonitrile and methyl ethyl ketone. Oxidation of the 5-hydroxymethyl group on the imidazole ring results in the active metabolite of losartan.
Losartan potassium is available as tablets for oral administration containing either 25 mg, 50 mg or 100 mg of losartan potassium and the following inactive ingredients: colloidal silicon dioxide, hydroxypropyl cellulose, hypromellose, lactose anhydrous, magnesium stearate, microcrystalline cellulose, pregelatinized starch, talc and titanium dioxide.
Losartan potassium 25 mg, 50 mg and 100 mg tablets contain potassium in the following amounts: 2.12 mg (0.054 mEq), 4.24 mg (0.108 mEq) and 8.48 mg (0.216 mEq), respectively.
[image: MM8]
Losartan potassium tablets, USP 25 mg, are white to off-white colored, oval shaped, biconvex, film coated tablets debossed with "25" on one side and "113" on the other side.
| Bottles of 90 |
NDC 13668-113-90 |
| Bottles of 1000 |
NDC 13668-113-10 |
| 100 Unit Dose Tablets |
NDC 13668-113-74 |
Losartan potassium tablets, USP 50 mg, are white to off-white colored, oval shaped, biconvex, film coated tablets debossed with "114" on one side and breakline on the other side.
| Bottles of 30 |
NDC 13668-409-30 |
| Bottles of 90 |
NDC 13668-409-90 |
| Bottles of 1000 |
NDC 13668-409-10 |
| 100 Unit Dose Tablets |
NDC 13668-409-74 |
Losartan potassium tablets, USP 100 mg, are white to off-white colored, oval shaped, biconvex, film coated tablets debossed with "100" on one side and "115" on the other side.
| Bottles of 30 |
NDC 13668-115-30 |
| Bottles of 90 |
NDC 13668-115-90 |
| Bottles of 1000 |
NDC 13668-115-10 |
| 100 Unit Dose Tablets |
NDC 13668-115-74 |
Storage
Store at 20°-25°C (68°-77°F); excursions permitted to 15°-30°C (59°-86°F). [see USP Controlled Room Temperature]. Keep container tightly closed. Protect from light.
Photos of the product and/or packaging supplied by the manufacturer.
Rx Only
Mechanism of Action
Angiotensin II [formed from angiotensin I in a reaction catalyzed by angiotensin converting enzyme (ACE, kininase II)], is a potent vasoconstrictor, the primary vasoactive hormone of the renin-angiotensin system and an important component in the pathophysiology of hypertension. It also stimulates aldosterone secretion by the adrenal cortex. Losartan and its principal active metabolite block the vasoconstrictor and aldosterone-secreting effects of angiotensin II by selectively blocking the binding of angiotensin II to the AT receptor found in many tissues, ( vascular smooth muscle, adrenal gland). There is also an AT receptor found in many tissues but it is not known to be associated with cardiovascular homeostasis. Both losartan and its principal active metabolite do not exhibit any partial agonist activity at the AT receptor and have much greater affinity (about 1000-fold) for the AT receptor than for the AT receptor. binding studies indicate that losartan is a reversible, competitive inhibitor of the AT receptor. The active metabolite is 10 to 40 times more potent by weight than losartan and appears to be a reversible, non-competitive inhibitor of the AT receptor. 1 e.g., 2 1 1 2 In vitro 1 1
Neither losartan nor its active metabolite inhibits ACE (kininase II, the enzyme that converts angiotensin I to angiotensin II and degrades bradykinin); nor do they bind to or block other hormone receptors or ion channels known to be important in cardiovascular regulation.
Pharmacokinetics
General
Losartan is an orally active agent that undergoes substantial first-pass metabolism by cytochrome P450 enzymes. It is converted, in part, to an active carboxylic acid metabolite that is responsible for most of the angiotensin II receptor antagonism that follows losartan treatment. Losartan metabolites have been identified in human plasma and urine. In addition to the active carboxylic acid metabolite, several inactive metabolites are formed. Following oral and intravenous administration of C-labeled losartan potassium, circulating plasma radioactivity is primarily attributed to losartan and its active metabolite. studies indicate that cytochrome P450 2C9 and 3A4 are involved in the biotransformation of losartan to its metabolites. Minimal conversion of losartan to the active metabolite (less than 1% of the dose compared to 14% of the dose in normal subjects) was seen in about one percent of individuals studied. 14 In vitro
The terminal half-life of losartan is about 2 hours and of the metabolite is about 6-9 hours.
The pharmacokinetics of losartan and its active metabolite are linear with oral losartan doses up to 200 mg and do not change over time. Neither losartan nor its metabolite accumulates in plasma upon repeated once-daily dosing.
Following oral administration, losartan is well absorbed (based on absorption of radiolabeled losartan) and undergoes substantial first-pass metabolism; the systemic bioavailability of losartan is approximately 33%. About 14% of an orally-administered dose of losartan is converted to the active metabolite. Mean peak concentrations of losartan and its active metabolite are reached in 1 hour and in 3-4 hours, respectively. While maximum plasma concentrations of losartan and its active metabolite are approximately equal, the AUC of the metabolite is about 4 times as great as that of losartan. A meal slows absorption of losartan and decreases its C but has only minor effects on losartan AUC or on the AUC of the metabolite (about 10% decreased). max
The pharmacokinetics of losartan and its active metabolite were also determined after IV doses of each component separately in healthy volunteers. The volume of distribution of losartan and the active metabolite is about 34 liters and 12 liters, respectively. Total plasma clearance of losartan and the active metabolite is about 600 mL/min and 50 mL/min, respectively, with renal clearance of about 75 mL/min and 25 mL/min, respectively. After single doses of losartan administered orally, about 4% of the dose is excreted unchanged in the urine and about 6% is excreted in urine as active metabolite. Biliary excretion contributes to the elimination of losartan and its metabolites. Following oral C-labeled losartan, about 35% of radioactivity is recovered in the urine and about 60% in the feces. Following an intravenous dose of C-labeled losartan, about 45% of radioactivity is recovered in the urine and 50% in the feces. 14 14
Both losartan and its active metabolite are highly bound to plasma proteins, primarily albumin, with plasma free fractions of 1.3% and 0.2%, respectively. Plasma protein binding is constant over the concentration range achieved with recommended doses. Studies in rats indicate that losartan crosses the blood-brain barrier poorly, if at all.
Special Populations
Pharmacokinetic parameters after multiple doses of losartan (average dose 0.7 mg/kg, range 0.36 to 0.97 mg/kg) as a tablet to 25 hypertensive patients aged 6 to 16 years are shown in Table 1 below. Pharmacokinetics of losartan and its active metabolite were generally similar across the studied age groups and similar to historical pharmacokinetic data in adults. The principal pharmacokinetic parameters in adults and children are shown in the table below. Pediatric:
Table 1 Pharmacokinetic Parameters in Hypertensive Adults and Children Age 6-16 Following Multiple Dosing
|
Mean ± standard deviation
a
Harmonic mean and standard deviation
b
Median
c
|
||||
|
|
Adults given 50 mg once daily for 7 days N=12
|
Age 6-16 given 0.7 mg/kg once daily for 7 days N=25
|
||
|
|
Parent
|
Active Metabolite
|
Parent
|
Active Metabolite
|
| AUC (ng•h/mL)
0
-
2
4
a
|
442 ± 173
|
1685 ± 452
|
368 ± 169
|
1866 ± 1076
|
| C (ng/mL)
m
a
x
a
|
224 ± 82
|
212 ± 73
|
141 ± 88
|
222 ± 127
|
| T (h)
½
b
|
2.1 ± 0.70
|
7.4 ± 2.4
|
2.3 ± 0.8
|
5.6 ± 1.2
|
| T (h)
p
e
a
k
c
|
0.9
|
3.5
|
2.0
|
4.1
|
| CL (mL/min)
r
e
n
a
|
56 ± 23
|
20 ± 3
|
53 ± 33
|
17 ± 8
|
The bioavailability of the suspension formulation was compared with losartan tablets in healthy adults. The suspension and tablet are similar in their bioavailability with respect to both losartan and the active metabolite (see ). , DOSAGE AND ADMINISTRATION Preparation of Suspension
Losartan pharmacokinetics have been investigated in the elderly (65-75 years) and in both genders. Plasma concentrations of losartan and its active metabolite are similar in elderly and young hypertensives. Plasma concentrations of losartan were about twice as high in female hypertensives as male hypertensives, but concentrations of the active metabolite were similar in males and females. No dosage adjustment is necessary (see Geriatric and Gender: ). DOSAGE AND ADMINISTRATION
Pharmacokinetic differences due to race have not been studied (see also and Race : , PRECAUTIONS Race , CLINICAL PHARMACOLOGY , , ). Pharmacodynamics and Clinical Effects Reduction in the Risk of Stroke Race
Following oral administration, plasma concentrations and AUCs of losartan and its active metabolite are increased by 50-90% in patients with mild (creatinine clearance of 50 to 74 mL/min) or moderate (creatinine clearance 30 to 49 mL/min) renal insufficiency. In this study, renal clearance was reduced by 55-85% for both losartan and its active metabolite in patients with mild or moderate renal insufficiency. Neither losartan nor its active metabolite can be removed by hemodialysis. No dosage adjustment is necessary for patients with renal impairment unless they are volume-depleted (see and Renal Insufficiency : , WARNINGS Hypotension ─ Volume-Depleted Patients ). DOSAGE AND ADMINISTRATION
Following oral administration in patients with mild to moderate alcoholic cirrhosis of the liver, plasma concentrations of losartan and its active metabolite were, respectively, 5-times and about 1.7-times those in young male volunteers. Compared to normal subjects the total plasma clearance of losartan in patients with hepatic insufficiency was about 50% lower and the oral bioavailability was about 2-times higher. A lower starting dose is recommended for patients with a history of hepatic impairment (see Hepatic Insufficiency : ). DOSAGE AND ADMINISTRATION
Drug Interactions
Losartan, administered for 12 days, did not affect the pharmacokinetics or pharmacodynamics of a single dose of warfarin. Losartan did not affect the pharmacokinetics of oral or intravenous digoxin. There is no pharmacokinetic interaction between losartan and hydrochlorothiazide. Coadministration of losartan and cimetidine led to an increase of about 18% in AUC of losartan but did not affect the pharmacokinetics of its active metabolite. Coadministration of losartan and phenobarbital led to a reduction of about 20% in the AUC of losartan and that of its active metabolite. A somewhat greater interaction (approximately 40% reduction in the AUC of active metabolite and approximately 30% reduction in the AUC of losartan) has been reported with rifampin. Fluconazole, an inhibitor of cytochrome P450 2C9, decreased the AUC of the active metabolite by approximately 40%, but increased the AUC of losartan by approximately 70% following multiple doses. Conversion of losartan to its active metabolite after intravenous administration is not affected by ketoconazole, an inhibitor of P450 3A4. The AUC of active metabolite following oral losartan was not affected by erythromycin, another inhibitor of P450 3A4, but the AUC of losartan was increased by 30%.
Pharmacodynamics and Clinical Effects
Losartan Potassium Tablets, USP
25mg, 50mg, 100mg
Rx only
Read the Patient Information that comes with losartan potassium tablets before you start taking it and each time you get a refill. There may be new information. This leaflet does not take the place of talking with your doctor about your condition and treatment.
What is the most important information I should know about losartan potassium tablets?
Do not take losartan potassium tablets if you are pregnant or plan to become pregnant. Losartan potassium tablets can harm your unborn baby causing injury and even death. Stop taking losartan potassium tablets if you become pregnant and call your doctor right away. If you plan to become pregnant, talk to your doctor about other treatment options before taking losartan potassium tablets.
What are losartan potassium tablets?
Losartan potassium tablets are prescription medicine called an angiotensin receptor blocker (ARB). It is used:
Losartan potassium tablets have not been studied in children less than 6 years old or in children with certain kidney problems.
High Blood Pressure (hypertension). Blood pressure is the force in your blood vessels when your heart beats and when your heart rests. You have high blood pressure when the force is too much. Losartan potassium tablets can help your blood vessels relax so your blood pressure is lower.
Left Ventricular Hypertrophy (LVH) is an enlargement of the walls of the left chamber of the heart (the heart’s main pumping chamber). LVH can happen from several things. High blood pressure is the most common cause of LVH.
Type 2 Diabetes with Nephropathy. Type 2 diabetes is a type of diabetes that happens mainly in adults. If you have diabetic nephropathy it means that your kidneys do not work properly because of damage from the diabetes.
Who should not take losartan potassium tablets?
What should I tell my doctor before taking losartan potassium tablets?
Tell your doctor about all of your medical conditions including if you:
Tell your doctor about all the medicines you take, including prescription and non-prescription medicines, vitamins, and herbal supplements. Losartan potassium tablets and certain other medicines may interact with each other. Especially tell your doctor if you are taking:
How should I take losartan potassium tablets?
What are the possible side effects of losartan potassium tablets?
Losartan potassium tablets may cause the following side effects that may be serious:
The most common side effects of losartan potassium tablets in people with high blood pressure are:
The most common side effects of losartan potassium tablets in people with type 2 diabetes with diabetic kidney disease are:
Tell your doctor if you get any side effect that bothers you or that won’t go away.
This is not a complete list of side effects. For a complete list, ask your doctor or pharmacist.
Call your doctor for medical advice about side effects. You may report side effects to FDA at 1-800-FDA-1088.
How do I store losartan potassium tablets?
General information about losartan potassium tablets
Medicines are sometimes prescribed for conditions that are not mentioned in patient information leaflets. Do not use losartan potassium tablets for a condition for which it was not prescribed. Do not give losartan potassium tablets to other people, even if they have the same symptoms that you have. It may harm them.
This leaflet summarizes the most important information about losartan potassium tablets. If you would like more information, talk with your doctor. You can ask your pharmacist or doctor for information about losartan potassium tablets that is written for health professionals.
What are the ingredients in losartan potassium tablets?
Active ingredients: losartan potassium, USP
Inactive ingredients: colloidal silicon dioxide, hydroxypropyl cellulose, hypromellose, lactose anhydrous, magnesium stearate, microcrystalline cellulose, pregelatinized starch, talc and titanium dioxide.
[image: MM7]
Manufactured by:
TORRENT PHARMACEUTICALS LTD., Indrad-382 721, Dist. Mehsana, INDIA.
For:
TORRENT PHARMA INC., 5380 Holiday Terrace, Suite 40, Kalamazoo, Michigan 49009.
8029683 Revised
July 2011
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