| Fact Table | |
|---|---|
| Formula | C9H15N5O |
| License | FDA approved (Loniten NDA 018154; original approval 1979); Health Canada marketed as Loniten 2.5 mg and 10 mg tablets |
| Bioavailability | At least 90% absorbed orally from the gastrointestinal tract |
| Legal status | Prescription only (Rx; oral tablets). Topical minoxidil =5% may be non-prescription in Canada |
| Chemical Name | 2,4-Pyrimidinediamine, 6-(1-piperidinyl)-, 3-oxide; 6-(piperidin-1-yl)pyrimidine-2,4-diamine 3-oxide |
| Elimination half-life | Approximately 4.2 hours; antihypertensive effect may persist for several days |
| Dosage (Strength) | 2.5 mg and 10 mg oral tablets; adults and children over 12 years: initial 5 mg once daily, usual effective range 10–40 mg/day, maximum 100 mg/day; usually given with a diuretic and beta-blocker or other sympathetic suppressant |
| Pregnancy | Pregnancy Category C in older labeling; use only if potential benefit justifies fetal risk. Neonatal hypertrichosis has been reported after exposure during pregnancy |
| Brands | Loniten; Minodyl; Rogaine/Regaine topical products; generic minoxidil oral tablets and topical solution/foam products |
| Protein binding | Does not bind to plasma proteins; negligible protein binding |
| PubChem CID | 4201 |
| MedlinePlus | a682608 |
| ChEBI | 6942 |
| ATC code | C02DC01; D11AX01 for topical dermatological minoxidil |
| DrugBank | DB00350 |
| KEGG | D00418 |
| Routes of administration | By mouth (oral tablets); topical cutaneous solution/foam for hair regrowth products |
Loniten (minoxidil) is a prescription oral drug used to treat severe high blood pressure when other medicines have not worked well. It relaxes and widens small blood vessels, making it easier for the heart to pump blood and lowering blood pressure. Because it can cause serious side effects, it is usually reserved for adults or children whose high blood pressure is dangerously high. Loniten tablets are not approved for hair loss.
Loniten is taken by mouth, usually once per day. Some people may split the dose into two doses if blood pressure drops too much after one dose.
Adults and children over 12 usually start with 5 mg once daily, and the dose may be increased slowly to 10 mg, 20 mg, or 40 mg per day as needed.
Most people take 10 to 40 mg per day, and the highest recommended dose is 100 mg per day.
Children under 12 are dosed by body weight, usually starting at 0.2 mg/kg once daily, with a maximum of 50 mg per day.
Doses are usually increased no more often than every 3 days, unless faster blood pressure control is needed.
Loniten is typically taken with other blood pressure medicines. Take it exactly as directed by a healthcare provider.
The active ingredient in Loniten is minoxidil. The inactive ingredients may include anhydrous lactose, colloidal silicon dioxide, magnesium stearate, microcrystalline cellulose, and sodium starch glycolate. Exact inactive ingredients may vary.
Before using this medication, you may want to consult a healthcare provider about the following:
Loniten carries a boxed warning about serious heart risks. It can cause fluid build-up around the heart (pericardial effusion), which can sometimes lead to a dangerous effect on the heart called cardiac tamponade. It can also worsen chest pain (angina) in people with coronary artery disease.
Loniten almost always needs to be taken with a diuretic (often a loop diuretic such as furosemide) to prevent fluid retention and to lower the risk of swelling, weight gain, and heart failure.
Loniten also needs to be taken with a beta-blocker or another medicine that slows the heart rate, since it raises the heart rate and can otherwise cause angina or increase stress on the heart.
Watch for signs of fluid build-up around the heart, including new or worsening shortness of breath, chest discomfort, swelling of the legs or abdomen, or unusual fatigue.
Loniten should not be given with guanethidine if at all possible, because the combination can cause severe drops in blood pressure when standing up.
Use with caution in people with kidney problems or those on dialysis, who often need lower doses and close monitoring.
Loniten has not been studied in people who had a heart attack within the past month, and it is generally avoided in that situation. Patients with severely high blood pressure should be started on Loniten in the hospital.
Increased body hair growth (hypertrichosis) is very common and not the same as scalp hair growth. It usually starts within 3 to 6 weeks of beginning therapy, often appearing on the temples, between the eyebrows, on the cheeks, and later on the arms, legs, and back. It is reversible and slowly fades over 1 to 6 months after stopping the medication.
Do not use Loniten oral tablets to try to treat hair loss. Only the topical minoxidil products are approved for hair growth.
Babies born to mothers who took minoxidil during pregnancy may be born with excess body hair (neonatal hypertrichosis). Minoxidil passes into breast milk and is generally not recommended while breastfeeding.
Avoid taking or using this medication if any of the following apply:
Common side effects of Loniten include:
Get medical help immediately for signs of fluid build-up around the heart or worsening heart function, such as new or worsening chest pain, shortness of breath, fast or irregular heartbeat, sudden swelling of the legs or abdomen, dizziness, or fainting.
Other serious problems can include pericarditis, pericardial effusion with tamponade, congestive heart failure from fluid overload, severe drops in blood pressure (especially when getting up), and signs of a serious allergic reaction such as rash, swelling of the face, lips, tongue, or throat, or trouble breathing.
A generic drug is a copy of the brand-name drug with the same dosage, safety, strength, quality, consumption method, performance, and intended use. Before generics become available on the market, the generic company must prove it has the same active ingredients as the brand-name drug and works in the same way and in the same amount of time in the body.
The only differences between generics and their brand-name counterparts is that generics are less expensive and may look slightly different (e.g., different shape or color), as trademark laws prevent a generic from looking exactly like the brand-name drug.
Generics are less expensive because generic manufacturers don't have to invest large sums of money to develop a drug. When the brand-name patent expires, generic companies can manufacture a copy of the brand-name and sell it at a substantial discount.