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Loniten®
minoxidil tablets, USPWARNINGSLONITEN Tablets contain the powerful antihypertensive agent, minoxidil, which may
produce serious adverse effects. It can cause pericardial effusion, occasionallyprogressing to tamponade, and angina pectoris may be exacerbated. LONITEN should bereserved for hypertensive patients who do not respond adequately to maximum
therapeutic doses of a diuretic and two other antihypertensive agents.
In experimental animals, minoxidil caused several kinds of myocardial lesions as well asother adverse cardiac effects (see Cardiac Lesions in Animals).
LONITEN must be administered under close supervision, usually concomitantly withtherapeutic doses of a beta-adrenergic blocking agent to prevent tachycardia andincreased myocardial workload. It must also usually be given with a diuretic, frequently
one acting in the ascending limb of the loop of Henle, to prevent serious fluid
accumulation. Patients with malignant hypertension and those already receiving
guanethidine (see WARNINGS) should be hospitalized when LONITEN is firstadministered so that they can be monitored to avoid too rapid, or large orthostatic,
decreases in blood pressure.
DESCRIPTIONLONITEN Tablets contain minoxidil, an antihypertensive peripheral vasodilator.
Minoxidil occurs as a white or off-white, odorless, crystalline solid that is soluble inwater to the extent of approximately 2 mg/mL, is readily soluble in propylene glycol or
ethanol, and is almost insoluble in acetone, chloroform or ethyl acetate. The chemicalname for minoxidil is 2,4-pyrimidinediamine,6-(1-piperidinyl)-, 3-oxide (mw=209.25).
The structural formula is represented at right:

LONITEN Tablets for oral administration contain either 2.5 mg or 10 mg of minoxidil.
Inactive ingredients: cellulose, corn starch, lactose, magnesium stearate, silicon dioxide.

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CLINICAL PHARMACOLOGY
1. General Pharmacologic Properties
Minoxidil is an orally effective direct acting peripheral vasodilator that reduces elevatedsystolic and diastolic blood pressure by decreasing peripheral vascular resistance.
Microcirculatory blood flow in animals is enhanced or maintained in all systemic
vascular beds. In man, forearm and renal vascular resistance decline; forearm blood flow
increases while renal blood flow and glomerular filtration rate are preserved.
Because it causes peripheral vasodilation, minoxidil elicits a number of predictable
reactions. Reduction of peripheral arteriolar resistance and the associated fall in bloodpressure trigger sympathetic, vagal inhibitory, and renal homeostatic mechanisms,
including an increase in renin secretion, that lead to increased cardiac rate and output andsalt and water retention. These adverse effects can usually be minimized by concomitantadministration of a diuretic and a beta-adrenergic blocking agent or other sympathetic
nervous system suppressant.
Minoxidil does not interfere with vasomotor reflexes and therefore does not produce
orthostatic hypotension. The drug does not enter the central nervous system inexperimental animals in significant amounts, and it does not affect CNS function in man.
2. Effects on Blood Pressure and Target Organs
The extent and time-course of blood pressure reduction by minoxidil do not correspondclosely to its concentration in plasma. After an effective single oral dose, blood pressure
usually starts to decline within one-half hour, reaches a minimum between 2 and 3 hours
and recovers at an arithmetically linear rate of about 30%/day. The total duration of effectis approximately 75 hours. When minoxidil is administered chronically, once or twice aday, the time required to achieve maximum effect on blood pressure with a given daily
dose is inversely related to the size of the dose. Thus, maximum effect is achieved on 10
mg/day within 7 days, on 20 mg/day within 5 days, and on 40 mg/day within 3 days.
The blood pressure response to minoxidil is linearly related to the logarithm of the dose
administered. The slope of this log-linear dose-response relationship is proportional to theextent of hypertension and approaches zero at a supine diastolic blood pressure of
approximately 85 mm Hg.
When used in severely hypertensive patients resistant to other therapy, frequently with anaccompanying diuretic and beta-blocker, LONITEN Tablets usually decreased the bloodpressure and reversed encephalopathy and retinopathy.
3. Absorption and Metabolism
Minoxidil is at least 90% absorbed from the GI tract in experimental animals and man.
Plasma levels of the parent drug reach maximum within the first hour and decline rapidly
thereafter. The average plasma half-life in man is 4.2 hours. Approximately 90% of theadministered drug is metabolized, predominantly by conjugation with glucuronic acid at
the N-oxide position in the pyrimidine ring, but also by conversion to more polar
products. Known metabolites exert much less pharmacologic effect than minoxidil itself;

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all are excreted principally in the urine. Minoxidil does not bind to plasma proteins anddoes not cross the blood brain barrier. Its renal clearance corresponds to the glomerular
filtration rate. In the absence of functional renal tissue, minoxidil and its metabolites canbe removed by hemodialysis.
4. Cardiac Lesions in Animals
Minoxidil produces several cardiac lesions in animals. Some are characteristic of agentsthat cause tachycardia and diastolic hypotension (beta-agonists like isoproterenol, arterial
dilators like hydralazine) while others are produced by a narrower range of agents witharterial dilating properties. The significance of these lesions for humans is not clear, as
they have not been recognized in patients treated with oral minoxidil at systemically
active doses, despite formal review of over 150 autopsies of treated patients.
(a) Papillary muscle/subendocardial necrosis
The most characteristic lesion of minoxidil, seen in rat, dog, and minipig (but notmonkeys) is focal necrosis of the papillary muscle and subendocardial areas of theleft ventricle. These lesions appear rapidly, within a few days of treatment withdoses of 0.5 to 10 mg/kg/day in the dog and minipig, and are not progressive,
although they leave residual scars. They are similar to lesions produced by otherperipheral arterial dilators, by theobromine, and by beta-adrenergic receptor
agonists such as isoproterenol, epinephrine, and albuterol. The lesions are thought
to reflect ischemia provoked by increased oxygen demand (tachycardia, increased
cardiac output) and relative decrease in coronary flow (decreased diastolicpressure and decreased time in diastole) caused by the vasodilatory effects ofthese agents coupled with reflex or directly induced tachycardia.
(b) Hemorrhagic lesions
After acute oral minoxidil treatment (0.5 to 10 mg/kg/day) in dogs and minipigs,
hemorrhagic lesions are seen in many parts of the heart, mainly in the epicardium,endocardium, and walls of small coronary arteries and arterioles. In minipigs thelesions occur primarily in the left atrium while in dogs they are most prominent in
the right atrium, frequently appearing as grossly visible hemorrhagic lesions. With
exposure of 1–20 mg/kg/day in the dog for 30 days or longer, there is replacementof myocardial cells by proliferating fibroblasts and angioblasts, hemorrhage andhemosiderin accumulation. These lesions can be produced by topical minoxidil
administration that gives systemic absorption of 0.5 to 1 mg/kg/day. Other
peripheral dilators, including an experimental agent, nicorandil, and theobromine,
have produced similar lesions.
(c) Epicarditis
A less fully studied lesion is focal epicarditis, seen in dogs after 2 days of oral
minoxidil. More recently, chronic proliferative epicarditis was observed in dogs
treated topically twice a day for 90 days. In a one year oral dog study,
serosanguinous pericardial fluid was seen.
(d) Hypertrophy and Dilation
Oral and topical studies in rats, dogs, monkeys (oral only), and rabbits (dermal
only) show cardiac hypertrophy and dilation. This is presumed to represent the3
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consequences of prolonged fluid overload; there is preliminary evidence inmonkeys that diuretics partly reverse these effects.
Autopsies of over 150 patients who died of various causes after receiving minoxidil for
hypertension have not revealed the characteristic hemorrhagic (especially atrial) lesions
seen in dogs and minipigs. While areas of papillary muscle and subendocardial necrosis
were occasionally seen, they occurred in the presence of known preexisting coronary
artery disease and were also seen in patients never exposed to minoxidil in another series
using similar, but not identical, autopsy methods.
INDICATIONS AND USAGE
Because of the potential for serious adverse effects, LONITEN Tablets are indicated onlyin the treatment of hypertension that is symptomatic or associated with target organ
damage and is not manageable with maximum therapeutic doses of a diuretic plus twoother antihypertensive drugs. At the present time use in milder degrees of hypertension is
not recommended because the benefit-risk relationship in such patients has not been
defined.
LONITEN reduced supine diastolic blood pressure by 20 mm Hg or to 90 mm Hg or lessin approximately 75% of patients, most of who had hypertension that could not be
controlled by other drugs.
CONTRAINDICATIONSLONITEN Tablets are contraindicated in pheochromocytoma, because it may stimulate
secretion of catecholamines from the tumor through its antihypertensive action.
LONITEN is contraindicated in those patients with a history of hypersensitivity to any of
the components of the preparation.
WARNINGS
1. Salt and Water Retention:
Congestive Heart Failure—concomitant use of an adequate diuretic is required—
LONITEN Tablets must usually be administered concomitantly with a diuretic adequate
to prevent fluid retention and possible congestive heart failure; a high ceiling (loop)
diuretic is almost always required. Body weight should be monitored closely. If
LONITEN is used without a diuretic, retention of several hundred milli-equivalents ofsalt and corresponding volumes of water can occur within a few days, leading toincreased plasma and interstitial fluid volume and local or generalized edema. Diuretic
treatment alone, or in combination with restricted salt intake, will usually minimize fluid
retention, although reversible edema did develop in approximately 10% of nondialysis
patients so treated. Ascites has also been reported. Diuretic effectiveness was limited
mostly by disease-related impaired renal function. The condition of patients with pre­existing congestive heart failure occasionally deteriorated in association with fluid
retention although because of the fall in blood pressure (reduction of afterload), morethan twice as many improved than worsened. Rarely, refractory fluid retention may
require discontinuation of LONITEN. Provided that the patient is under close medical
supervision, it may be possible to resolve refractory salt retention by discontinuing

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LONITEN for 1 or 2 days and then resuming treatment in conjunction with vigorous
diuretic therapy.
2. Concomitant Treatment to Prevent Tachycardia is Usually Required—
LONITEN increases the heart rate. Angina may worsen or appear for the first time during
LONITEN treatment, probably because of the increased oxygen demands associated withincreased heart rate and cardiac output. The increase in rate and the occurrence of angina
generally can be prevented by the concomitant administration of a beta-adrenergic
blocking drug or other sympathetic nervous system suppressant. The ability of beta­
adrenergic blocking agents to minimize papillary muscle lesions in animals is further
reason to utilize such an agent concomitantly. Round-the-clock effectiveness of thesympathetic suppressant should be ensured.
3. Pericarditis, Pericardial Effusion and Tamponade—There have been reportsof pericarditis occurring in association with the use of LONITEN. The relationship of thisassociation to renal status is uncertain. Pericardial effusion, occasionally with tamponade,has been observed in about 3% of treated patients not on dialysis, especially those withinadequate or compromised renal function. Although in many cases, the pericardial
effusion was associated with a connective tissue disease, the uremic syndrome,congestive heart failure, or marked fluid retention, there have been instances in whichthese potential causes of effusion were not present. Patients should be observed closely
for any suggestion of a pericardial disorder, and echocardiographic studies should be
carried out if suspicion arises. More vigorous diuretic therapy, dialysis,
pericardiocentesis, or surgery may be required. If the effusion persists, withdrawal of
LONITEN should be considered in light of other means of controlling the hypertension
and the patient’s clinical status.
4. Interaction with Guanethidine:
Although minoxidil does not itself cause orthostatic hypotension, its administration topatients already receiving guanethidine can result in profound orthostatic effects. If at all
possible, guanethidine should be discontinued well before minoxidil is begun. Where thisis not possible, minoxidil therapy should be started in the hospital and the patient should
remain institutionalized until severe orthostatic effects are no longer present or the patient
has learned to avoid activities that provoke them.
5. Hazard of Rapid Control of Blood Pressure:
In patients with very severe blood pressure elevation, too rapid control of blood pressure,especially with intravenous agents, can precipitate syncope, cerebrovascular accidents,
myocardial infarction and ischemia of special sense organs with resulting decrease or lossof vision or hearing. Patients with compromised circulation or cryoglobulinemia may also
suffer ischemic episodes of the affected organs. Although such events have not beenunequivocally associated with minoxidil use, total experience is limited at present.
Any patient with malignant hypertension should have initial treatment with minoxidil
carried out in a hospital setting, both to assure that blood pressure is falling and to assurethat it is not falling more rapidly than intended.

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PRECAUTIONS
1. General Precautions(a) Monitor fluid and electrolyte balance and body weight (see WARNINGS:
Salt and Water Retention).
(b) Observe patients for signs and symptoms of pericardial effusion (seeWARNINGS: Pericarditis, Pericardial Effusion, and Tamponade).
(c) Use after myocardial infarction—LONITEN Tablets have not been used inpatients who have had a myocardial infarction within the preceding month. It is
possible that a reduction of arterial pressure with LONITEN might further limit
blood flow to the myocardium, although this might be compensated by decreased
oxygen demand because of lower blood pressure.
(d) Hypersensitivity—Possible hypersensitivity to LONITEN, manifested as a skinrash, has been seen in less than 1% of patients; whether the drug should be
discontinued when this occurs depends on treatment alternatives.
(e) Renal failure or dialysis—Patients may require smaller doses of LONITEN andshould have close medical supervision to prevent exacerbation of renal failure or
precipitation of cardiac failure.
2. Information for Patient
The patient should be fully aware of the importance of continuing all of his
antihypertensive medications and of the nature of symptoms that would suggest fluid
overload. A patient brochure has been prepared and is included with each LONITEN
package. The text of this brochure is reprinted at the end of the insert.
3. Laboratory Tests
Those laboratory tests which are abnormal at the time of initiation of minoxidil therapy,
such as urinalysis, renal function tests, EKG, chest x-ray, echocardiogram, etc., should be
repeated at intervals to ascertain whether improvement or deterioration is occurring underminoxidil therapy. Initially such tests should be performed frequently, eg, 1–3 monthintervals; later as stabilization occurs, at intervals of 6–12 months.
4. Drug interactions
See "Interaction with Guanethidine" under WARNINGS.
5. Carcinogenesis, Mutagenesis and Impairment of Fertility—Two-year
carcinogenicity studies of minoxidil have been conducted by the dermal and oral (dietary)routes of administration in mice and rats. There were no positive findings with the oral
(dietary) route of administration in rats.
In the two-year dermal study in mice, an increased incidence of mammary adenomas andadenocarcinomas in the females at all dose levels (8, 25 and 80 mg/kg/day) was attributed
to increased prolactin activity. Hyperprolactinemia is a well-known mechanism in theenhancement of mouse mammary tumors, but has not been associated with mammary
tumorigenesis in women. Additionally, topical minoxidil has not been shown to cause
hyperprolactinemia in women on clinical trials. Absorption of minoxidil through rodent

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skin is greater than would be experienced by patients treated topically with minoxidil forhair loss. Dietary administration of minoxidil to mice for up to 2 years was associatedwith an increased incidence of malignant lymphomas in females at all dose levels (10, 25
and 63 mg/kg/day) and an increased incidence of hepatic nodules in males (63mg/kg/day). There was no effect of dietary minoxidil on the incidence of malignant liver
tumors.
In the two-year dermal study in rats there were significant increases in incidence ofpheochromocytomas in males and females and preputial gland adenomas in males.
Changes in incidence of neoplasms found to be increased in the dermal or oral
carcinogenicity studies were typical of those expected in rodents treated with otherhypotensive agents (adrenal pheochromocytomas in rats), treatment-related hormonal
alterations (mammary carcinomas in female mice; preputial gland adenomas in male rats)or representative of normal variations within the range of historical incidence for rodent
neoplasms (malignant lymphomas, liver nodules/adenomas in mice). Based on
differences in absorption of minoxidil and mechanisms of tumorigenesis in these rodent
species, none of these changes were considered to be relevant to the safety of patientstreated topically with minoxidil for hair loss.
There was no evidence of epithelial hyperplasia or tumorigenesis at the sites of topicalapplication of minoxidil in either species in the 2-year dermal carcinogenesis studies. No
evidence of carcinogenicity was detected in rats or rabbits treated topically withminoxidil for one year. Topical minoxidil (2% and 5%) did not significantly (p<0.05)
reduce the latency period of UV light-initiated skin tumors in hairless mice, as compared
to controls, in a 12-month photocarcinogenicity study.
Minoxidil was not mutagenic in the Salmonella (Ames) test, the DNA damage alkaline
elution assay, the in vitro rat hepatocyte unscheduled DNA synthesis (UDS) assay, the rat
bone marrow micronucleus assay, or the mouse bone marrow micronucleus assay. An
equivocal result was recorded in an in vitro cytogenetic assay using Chinese hamster cells
at long exposure times, but a similar assay using human lymphocytes was negative.
In a study in which male and female rats received one or five times the maximum
recommended human oral antihypertensive dose of minoxidil (multiples based on a 50 kg
patient) there was a dose-dependent reduction in conception rate.
6. Pregnancy
Teratogenic Effects
Pregnancy Category C. Oral administration of minoxidil has been associated withevidence of increased fetal resorption in rabbits, but not rats, when administered at fivetimes the maximum recommended oral antihypertensive human dose. There was noevidence of teratogenic effects in rats and rabbits. Subcutaneous administration ofminoxidil to pregnant rats at 80 mg/kg/day was maternally toxic but not teratogenic.
Higher subcutaneous doses produced evidence of developmental toxicity. There are noadequate and well controlled studies in pregnant women. LONITEN should be usedduring pregnancy only if the potential benefit justifies the potential risk to the fetus.

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Neonatal hypertrichosis has been reported following exposure to minoxidil during
pregnancy.
7. Labor and Delivery
The effects on labor and delivery are unknown.
8. Nursing Mothers
There has been one report of minoxidil excretion in the breast milk of a woman treatedwith 5 mg oral minoxidil twice daily for hypertension. Because of the potential foradverse effects in nursing infants from minoxidil absorption, LONITEN should not be
administered to a nursing woman.
9. Pediatric Use
Use in pediatric patients has been limited to date, particularly in infants. The
recommendations under DOSAGE AND ADMINISTRATION can be considered only arough guide at present and a careful titration is essential.
10. Geriatric Use
Clinical studies of LONITEN Tablets did not include sufficient numbers of subjects aged
65 and over to determine whether they respond differently from younger subjects. Other
reported clinical experience has not identified differences in responses between theelderly and younger patients. In general, dose selection for an elderly patient should becautious, usually starting at the low end of the dosing range, reflecting the greater
frequency of decreased hepatic, renal, or cardiac function, and of concomitant disease orother drug therapy.
11. Unapproved Use
Use of LONITEN Tablets, in any formulation, to promote hair growth is not an approved
indication. While clinical trials with ROGAINE® Topical Solution 2% demonstrated that
formulation and dosage were safe and effective, the effects of extemporaneous
formulations and dosages have not been shown to be safe or effective. Because systemic
absorption of topically applied drug may occur and is dependent on vehicle and/or
method of use, extemporaneous topical formulations made from LONITEN should beconsidered to share in the full range of CONTRAINDICATIONS, WARNINGS,
PRECAUTIONS, and ADVERSE REACTIONS listed in this insert. In addition, skinintolerance to drug and/or vehicle may occur.
ADVERSE REACTIONS
1. Salt and Water Retention (see WARNINGS: Concomitant Use of Adequate
Diuretic is Required)—Temporary edema developed in 7% of patients who were notedematous at the start of therapy.
2. Pericarditis, Pericardial Effusion and Tamponade (see WARNINGS).
3. Dermatologic—Hypertrichosis—Elongation, thickening, and enhanced pigmentationof fine body hair are seen in about 80% of patients taking LONITEN Tablets. This
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develops within 3 to 6 weeks after starting therapy. It is usually first noticed on thetemples, between the eyebrows, between the hairline and the eyebrows, or in the sideburn area of the upper lateral cheek, later extending to the back, arms, legs, and scalp.
Upon discontinuation of LONITEN, new hair growth stops, but 1 to 6 months may berequired for restoration to pretreatment appearance. No endocrine abnormalities havebeen found to explain the abnormal hair growth; thus, it is hypertrichosis without
virilism. Hair growth is especially disturbing to children and women and such patientsshould be thoroughly informed about this effect before therapy with LONITEN is begun.
Allergic—Rashes have been reported, including rare reports of bullous eruptions, toxic
epidermal necrolysis, and Stevens-Johnson Syndrome.
4. Hematologic—Thrombocytopenia and leukopenia (WBC<3000/mm3) have rarely
been reported.
5. Gastrointestinal—Nausea and/or vomiting has been reported. In clinical trials theincidence of nausea and vomiting associated with the underlying disease has shown adecrease from pretrial levels.
6. Miscellaneous—Breast tenderness—This developed in less than 1% of patients.
7. Altered Laboratory Findings — (a) ECG changes—Changes in direction andmagnitude of the ECG T-waves occur in approximately 60% of patients treated withLONITEN. In rare instances a large negative amplitude of the T-wave may encroach
upon the S-T segment, but the S-T segment is not independently altered. These changes
usually disappear with continuance of treatment and revert to the pretreatment state if
LONITEN is discontinued. No symptoms have been associated with these changes, norhave there been alterations in blood cell counts or in plasma enzyme concentrations thatwould suggest myocardial damage. Long-term treatment of patients manifesting suchchanges has provided no evidence of deteriorating cardiac function. At present thechanges appear to be nonspecific and without identifiable clinical significance. (b)Effects of hemodilution—hematocrit, hemoglobin and erythrocyte count usually fall
about 7% initially and then recover to pretreatment levels. (c) Other—Alkaline
phosphatase increased varyingly without other evidence of liver or bone abnormality.
Serum creatinine increased an average of 6% and BUN slightly more, but later declined
to pretreatment levels.
OVERDOSAGE
There have been only a few instances of deliberate or accidental overdosage withLONITEN Tablets. One patient recovered after taking 50 mg of minoxidil together with
500 mg of a barbiturate. When exaggerated hypotension is encountered, it is most likely
to occur in association with residual sympathetic nervous system blockade from previous
therapy (guanethidine-like effects or alpha-adrenergic blockage), which prevents theusual compensatory maintenance of blood pressure. Intravenous administration of normal
saline will help to maintain blood pressure and facilitate urine formation in these patients.
Sympathomimetic drugs such as norepinephrine or epinephrine should be avoided

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because of their excessive cardiac stimulating action. Phenylephrine, angiotensin II,
vasopressin, and dopamine all reverse hypotension due to LONITEN, but should only be
used if underperfusion of a vital organ is evident.
Radioimmunoassay can be performed to determine the concentration of minoxidil in the
blood. At the maximum adult dose of 100 mg/day, peak blood levels of 1641 ng/mL and2441 ng/mL were observed in two patients, respectively. Due to patient-to-patientvariation in blood levels, it is difficult to establish an overdosage warning level. In
general, a substantial increase above 2000 ng/mL should be regarded as overdosage,
unless the physician is aware that the patient has taken no more than the maximum dose.
Oral LD50 in rats has ranged from 1321 – 3492 mg/kg; in mice, 2456 – 2648 mg/kg.
DOSAGE AND ADMINISTRATION
Patients over 12 years of age: The recommended initial dosage of LONITEN
Tablets is 5 mg of minoxidil given as a single daily dose. Daily dosage can be increased
to 10, 20 and then to 40 mg in single or divided doses if required for optimum bloodpressure control. The effective dosage range is usually 10 to 40 mg per day. The
maximum recommended dosage is 100 mg per day.
Patients under 12 years of age: The initial dosage is 0.2 mg/kg minoxidil as a single
daily dose. The dosage may be increased in 50 to 100% increments until optimum bloodpressure control is achieved. The effective dosage range is usually 0.25 to 1.0 mg/kg/day.
The maximum recommended dosage is 50 mg daily (see 9. Pediatric Use under
PRECAUTIONS).
Dose frequency: The magnitude of within-day fluctuation of arterial pressure during
therapy with LONITEN is directly proportional to the extent of pressure reduction. If
supine diastolic pressure has been reduced less than 30 mm Hg, the drug need beadministered only once a day; if supine diastolic pressure has been reduced more than 30
mm Hg, the daily dosage should be divided into two equal parts.
Frequency of dosage adjustment: Dosage must be titrated carefully according toindividual response. Intervals between dosage adjustments normally should be at least 3days since the full response to a given dose is not obtained for at least that amount oftime. Where a more rapid management of hypertension is required, dose
adjustments can be made every 6 hours if the patient is carefully monitored.
Concomitant therapy: Diuretic and beta-blocker or other sympathetic nervous system
suppressant.
Diuretics: LONITEN must be used in conjunction with a diuretic in patients relying on
renal function for maintaining salt and water balance. Diuretics have been used at thefollowing dosages when starting therapy with LONITEN: hydrochlorothiazide (50 mg,
b.i.d.) or other thiazides at equieffective dosage; chlorthalidone (50 to 100 mg, once
daily); furosemide (40 mg, b.i.d.). If excessive salt and water retention results in a weight

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gain of more than 5 pounds, diuretic therapy should be changed to furosemide; if thepatient is already taking furosemide, dosage should be increased in accordance with thepatient’s requirements.
Beta-blocker or other sympathetic nervous system suppressants: Whentherapy with LONITEN is begun, the dosage of a beta-adrenergic receptor blocking drug
should be the equivalent of 80 to 160 mg of propranolol per day in divided doses.
If beta-blockers are contraindicated, methyldopa (250 to 750 mg, b.i.d.) may be usedinstead. Methyldopa must be given for at least 24 hours before starting therapy withLONITEN because of the delay in the onset of methyldopa’s action. Limited clinicalexperience indicates that clonidine may also be used to prevent tachycardia induced by
LONITEN; the usual dosage is 0.1 to 0.2 mg twice daily.
Sympathetic nervous system suppressants may not completely prevent an increase inheart rate due to LONITEN but usually do prevent tachycardia. Typically, patients
receiving a beta-blocker prior to initiation of therapy with LONITEN have a bradycardia
and can be expected to have an increase in heart rate toward normal when LONITEN is
added. When treatment with LONITEN and beta-blocker or other sympathetic nervous
system suppressant are begun simultaneously, their opposing cardiac effects usuallynullify each other, leading to little change in heart rate.
HOW SUPPLIEDLONITEN Tablets are available as follows:
2.5 mg (white, round, scored, imprinted U/121 and 2½)
Bottles of 100
NDC 0009-0121-01
10 mg (white, round, scored, imprinted LONITEN 10)
Bottles of 100
NDC 0009-0137-01
Store at controlled room temperature 20° to 25°C (68° to 77°F) [see USP].

LAB-0168-0.x
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PATIENT INFORMATIONLONITEN Tablets contain minoxidil, a medicine for the treatment of high blood pressurein the patient who has not been controlled or is experiencing unacceptable side effects
with other medications. It must usually be taken with other medicines.
Be absolutely sure to take all of your medicines for high blood pressure according to yourdoctor’s instructions. Do not stop taking LONITEN unless your doctor tells you to. Do
not give any of your medicine to other people.
It is important that you look for the warning signals of certain undesired effects of
LONITEN. Call your doctor if they occur. Your doctor will need to see you regularly
while you are taking LONITEN. Be sure to keep all your appointments or to arrange for
new ones if you must miss one.
Do not hesitate to call your doctor if any discomforts or problems occur.
The information here is intended to help you take LONITEN properly. It does not tell you
all there is to know about LONITEN. There is a more technical leaflet that you may
request from the pharmacist; you may need your doctor’s help in understanding parts ofthat leaflet.
What is LONITEN?
LONITEN Tablets contain minoxidil which is a drug for lowering the blood pressure. It
works by relaxing and enlarging certain small blood vessels so that blood flows throughthem more easily.

Why lower blood pressure?
Your doctor has prescribed LONITEN to lower your blood pressure and protect vital
parts of your body. Uncontrolled blood pressure can cause stroke, heart failure, blindness,kidney failure, and heart attacks.

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Most people with high blood pressure need to take medicines to treat it for their whole
lives.
Who should take LONITEN?
There are many people with high blood pressure, but most of them do not need
LONITEN. LONITEN is used ONLY when your doctor decides that:
1. your high blood pressure is severe;
2. your high blood pressure is causing symptoms or damage to vital organs; and3. other medicines did not work well enough or had very disturbing side effects.

LONITEN should be taken only when a doctor prescribes it. Never give any of your
LONITEN Tablets, or any other high blood pressure medicine, to a friend or relative.
Pregnancy: In some cases doctors may prescribe LONITEN for women who are
pregnant or who are planning to have children. However, its safe use in pregnancy has
not been established. Laboratory animals had a reduced ability to become pregnant and areduced survival of offspring while taking LONITEN. If you are pregnant or are planningto become pregnant, be sure to tell your doctor.
How to take LONITEN.
Usually, your doctor will prescribe two other medicines along with LONITEN. These
will help lower blood pressure and will help prevent undesired effects of LONITEN.
Often, when a medicine like LONITEN lowers blood pressure, your body tries to returnthe blood pressure to the original higher level. It does this by holding on to water and salt
(so there will be more fluid to pump) and by making your heart beat faster. To prevent
this, your doctor will usually prescribe a water tablet to remove the extra salt and waterfrom your body (a diuretic: dye-u-RET-tic) and another medicine to slow your heart beat.

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You must follow your doctor’s instructions exactly, taking all the prescribed
medicines, in the right amounts, each day. These medicines will help keep your bloodpressure down. The water tablet and heart beat medicine will help prevent the undesired
effects of LONITEN.
LONITEN Tablets come in two strengths (2½ milligrams and 10 milligrams) that aremarked on each tablet. Pay close attention to the tablet markings to be sure you are taking
the correct strength. Your doctor may prescribe half a tablet; the tablets are scored (partly
cut on one side) so that you can easily break them.

When you first start taking LONITEN, your doctor may need to see you often in order toadjust your dosage. Take all your medicine according to the schedule prescribed by yourdoctor. Do not skip any doses. If you should forget a dose of LONITEN, wait until it
is time for your next dose, then continue with your regular schedule. Remember: donot stop taking LONITEN, or any of your other high blood pressure medicines,
without checking with your doctor. Make sure that any doctor treating or examining
you knows that you are taking high blood pressure medicines, including LONITEN.
WARNING SIGNALS
Even if you take all your medicines correctly, LONITEN Tablets may cause undesired
effects. Some of these are serious and you should be on the lookout for them. If any of
the following warning signals occur, you must call your doctor immediately:
1. Increase in heart rate—You should measure your heart rate by counting your pulse
rate while you are resting. If you have an increase of 20 beats or more a minute overyour normal pulse, contact your doctor immediately. If you do not know how to take yourpulse rate, ask your doctor. Also ask your doctor how often to check your pulse.

2. Rapid weight gain of more than 5 pounds—You should weigh yourself daily. If you
quickly gain five or more pounds, or if there is any swelling or puffiness in the face,hands, ankles, or stomach area, this could be a sign that you are retaining body fluids.
Your doctor may have to change your drugs or change the dose of your drugs. You may
also need to reduce the amount of salt you eat. A smaller weight gain (2 to 3 pounds)
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often occurs when treatment is started. You may lose this extra weight with continued
treatment.

3. Increased difficulty in breathing, especially when lying down. This too may be due
to an increase of body fluids. I t can also happen because your high blood pressure isgetting worse. In either case, you might require treatment with other medicines.

4. New or worsening of pain in the chest, arm, or shoulder or signs of severe
indigestion—These could be signs of serious heart problems.

5. Dizziness, lightheadedness or fainting—These can be signs of high blood pressure or
they may be side effects from one of the medicines. Your doctor may need to change or
adjust the dosage of the medicines you are taking.

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OTHER UNDESIRED EFFECTSLONITEN Tablets can cause other undesired effects such as nausea and/or vomiting thatare annoying but not dangerous. Do not stop taking the drug because of these other
undesired effects without talking to your doctor.
Hair growth: About 8 out of every 10 patients who have taken LONITEN noticed thatfine body hair grew darker or longer on certain parts of the body. This happened about
3 to 6 weeks after beginning treatment. The hair may first be noticed on the forehead andtemples, between the eyebrows, or on the upper part of the cheeks. Later, hair may growon the back, arms, legs, or scalp. Although hair growth may not be noticeable to somepatients, it often is bothersome in women and children. Unwanted hair can becontrolled with a hair remover or by shaving. The extra hair is not permanent, it
disappears within 1 to 6 months of stopping LONITEN. Nevertheless, you should notstop taking LONITEN without first talking to your doctor.
A few patients have developed a rash or breast tenderness while taking LONITEN
Tablets, but this is unusual.

LAB-0169-0.x
Revised January 201516
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