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minoxidil (Loniten, Minodyl, Minoxidil HTN)

 

Classes: Vasodilators

Dosing and uses of Loniten, Minodyl (minoxidil)

 

Adult dosage forms and strengths

tablet

  • 2.5mg
  • 10mg

 

Severe or Refractory Hypertension (HTN)

Initial: 5mg PO qDay, increase every 3 days PRn

Maintenance: 2.5-80 mg/day qDay or q12hr; not to exceed 100 mg/day

 

Pediatric dosage forms and strengths

tablet

  • 2.5mg
  • 10mg

 

Severe or Refractory Hypertension (HTN)

< 12 years

  • Initial: 0.1-0.2 mg/kg; not to exceed 5 mg/day PO; titrate to response every 3 days
  • 0.25-1 mg/kg/day PO qDay or q12hr; not to exceed 50 mg/day

> 12 years

  • Initial: 5mg PO qDay, increase every 3 days PRN
  • Maintenance: 2.5-80 mg/day qDay or q12hr; not to exceed 100 mg/day

 

Geriatric dosage forms and strengths

 

Hypertension

2.5 mg PO qDay; titrate to response gradually

 

Loniten, Minodyl (minoxidil) adverse (side) effects

>10%

Hypertrichosis (80%)

Abnormal ECG (60%)

 

1-10%

Pericardial effusion (3%)

 

Frequency not defined

Angina

Cardiac tamponade

Fluid and sodium retention

Hypotension

Pericarditis

Tachyarrhythmia

Stevens-Johnson syndrome (rare )

Hirsutism

Leukopenia (rare)

Thrombocytopenia (rare)

Toxic epidermal necrolysis

 

Warnings

Black box warnings

Can precipitate effusion, occasionally progressing to tamponade

May exacerbate angina pectoris

Reserve for patients who do not respond adequately to maximum therapeutic doses of a diuretic and 2 other antihypertensives

In experimental animals, minoxidil caused several kinds of myocardial lesions as well as other adverse cardiac effects

Must be administered under close supervision, usually concomitantly with therapeutic doses of a beta-adrenergic blocking agent to prevent tachycardia and increased myocardial workload

Usually given with a diuretic (typically loop diuretic) to prevent serious fluid accumulation

Patients with malignant hypertension and those already receiving guanethidine should be hospitalized when minoxidil first administered (monitoring required because risk for rapid/large decrease in BP)

 

Contraindications

Hypersensitivity to minoxidiL

Pheochromocytoma

 

Cautions

Use with B-blocker or centrally-acting drug and a diuretic

Reserve for severe hypertension refractory to other drugs

Pericarditis and pericardial effusion with tamponade reported; observe patients closely for any suggestion of cardiac disorder; perform echocardiographic studies if cardiac disorder suspected; may treat with diureticsdialysis, pericardiocentesis or surgery; discontinue therapy if effusion persists

In patients with 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 loss of vision or hearing; patients with compromised circulation or cryoglobulinemia may also suffer ischemic episodes of affected organs

Patients 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 assure that it is not falling more rapidly than intended

Tablets have not been used in patients who have had a myocardial infarction within preceding month; use caution

Neonatal hypertrichosis reported following exposure to minoxidil during pregnancy

May exacerbate heart failure

 

Pregnancy and lactation

Pregnancy category: C

Lactation: controversial; excreted in breast milk, not recommended for long term use if breastfeeding

 

Pregnancy categories

A: Generally acceptable. Controlled studies in pregnant women show no evidence of fetal risk.

B: May be acceptable. Either animal studies show no risk but human studies not available or animal studies showed minor risks and human studies done and showed no risk.

C: Use with caution if benefits outweigh risks. Animal studies show risk and human studies not available or neither animal nor human studies done.

D: Use in LIFE-THREATENING emergencies when no safer drug available. Positive evidence of human fetal risk.

X: Do not use in pregnancy. Risks involved outweigh potential benefits. Safer alternatives exist.

NA: Information not available.

 

Pharmacology of Loniten, Minodyl (minoxidil)

Mechanism of action

Direct vasodilator; dilate arterioles with little effect on vein, decreases systemic resistance, which subsequently decreases blood pressure.

 

Pharmacokinetics

Half-Life: 4 hr

Excretion: Urine (12% as unchanged drug)

Duration: 2-5 Days

Peak Plasma Time: PO (HTN): 1 hr

Bioavailability: PO (HTN): 90%

Protein Bound: Negligible

Metabolism: liver, 88% via glucuronidation

Metabolite: minoxidil-0-glucuronide (active)

Onset

  • Initial effect: PO (HTN): 30-60 min
  • Max effect: PO (HTN): 4-8 hr