Piloxidil
Piloxidil Uses, Dosage, Side Effects, Food Interaction and all others data.
Piloxidil stimulates hair growth by increasing oxygen, blood and nutrients supply to the hair follicle by widening blood vessels and inhibiting androgen hormone to affect hair follicles.
Following topical application, an average of about 1.4% of the total applied dose is absorbed from the normal intact scalp. Topical Piloxidil absorption is increased by increasing the dose applied, increasing the frequency of dosing and decreasing the barrier function of the stratum corneum. Serum Piloxidil levels and systemic effects resulting from the administration of topical Piloxidil are governed by the drug’s absorption rate through the skin. Following cessation of topical dosing, approximately 95% of the systemically absorbed drug is eliminated within 4 days. Piloxidil and its metabolites are excreted principally in the urine.
Piloxidil is an orally effective direct acting peripheral vasodilator that reduces elevated systolic and diastolic blood pressure by decreasing peripheral vascular resistance. Piloxidil is also used topically to treat androgenetic alopecia. 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. The predominant site of minoxidil action is arterial. Venodilation does not occur with minoxidil; thus, postural hypotension is unusual with its administration. The antihypertensive activity of minoxidil is due to its sulphate metabolite, minoxidil sulfate.
| Trade Name | Piloxidil |
| Availability | Prescription only |
| Generic | Minoxidil |
| Minoxidil Other Names | Minossidile, Minoxidil, Minoxidilum |
| Related Drugs | amlodipine, lisinopril, metoprolol, losartan, furosemide, hydrochlorothiazide |
| Type | |
| Formula | C9H15N5O |
| Weight | Average: 209.2483 Monoisotopic: 209.127660127 |
| Protein binding | Minoxidil does not bind to plasma proteins. |
| Groups | Approved, Investigational |
| Therapeutic Class | Other scalp preparations |
| Manufacturer | |
| Available Country | Poland |
| Last Updated: | September 19, 2023 at 7:00 am |
Uses
Piloxidil is used for the treatment of androgenic alopecia in males and females and stabilisation of hair loss in patients with androgenic alopecia, and also of alopecia areata.
Piloxidil is also used to associated treatment for these conditions: Androgenetic Alopecia, Severe, symptomatic Hypertension
How Piloxidil works
Piloxidil is thought to promote the survival of human dermal papillary cells (DPCs) or hair cells by activating both extracellular signal-regulated kinase (ERK) and Akt and by preventing cell death by increasing the ratio of BCl-2/Bax. Piloxidil may stimulate the growth of human hairs by prolonging anagen through these proliferative and anti-apoptotic effects on DPCs. Piloxidil, when used as a vasodilator, acts by opening adenosine triphosphate-sensitive potassium channels in vascular smooth muscle cells. This vasodilation may also improve the viability of hair cells or hair follicles.
Dosage
Piloxidil dosage
Piloxidil topical solution is for external use only and should be applied when the hair and scalp are clean and dry. Apply 1 ml (7 sprays) of Piloxidil topical solution twice daily at 12-hour intervals to the scalp, beginning at the centre of the affected area and spreading the solution out to cover the entire affected area. The total daily application dose should not exceed 2 ml.
For the best results, Piloxidil topical solution should be allowed to remain on the scalp for about 4 hours before washing. The night-time application should be done 2-4 hours before going to bed to allow the solution to dry out. Piloxidil topical solution should not be massaged into the scalp, but applied lightly. A hair dryer should not be used to speed up the drying of the solution as it may decrease the effectiveness. Piloxidil topical solution should not be mixed with any hair oil. The drug should not be used more than two times a day, or be taken orally or applied to any other part of the body to avoid the risk of adverse effects and unwanted hair growth. More frequent use or longer application time have no effect on hair growth. In case of missing any daily applications of Piloxidil topical solution, the patient should continue with the next application.
Hands should be washed immediately if Piloxidil topical solution is applied with the fingertips. Clinical experience with Piloxidil indicates that twice-daily applications for 4 months or more may be required before there is evidence of hair growth. To arresthair fall, Piloxidil topical solution should be used for not less than 45 days. Depending upon the severity of hair loss or type and extent of baldness, particular strength of Piloxidil topical solution may be selected.
Side Effects
Commonly encountered side effects in clinical trials with Piloxidil topical solution were minor dermatological reactions. Dermatitis or hypertrichosis may occur. These incidences may occur in 0.1–5% of patients.
Toxicity
Oral LD50 in rats has ranged from 1321-3492 mg/kg; in mice, 2456-2648 mg/kg. Side effects include cardiovascular effects associated with hypotension such as sudden weight gain, rapid heart beat, faintness or dizziness.
Precaution
Piloxidil topical solution is more likely to cause scalp irritation. If scalp irritation continues or worsen, use of Piloxidil topical solution should be stopped.
Interaction
Piloxidil topical solution should not be used along with other topical agents known to alter the stratum corneum barrier such as tretinoin or dithranol, due to the enhanced absorption of Piloxidil. Although there is no clinical evidence, there exists the theoretical possibility of absorbed Piloxidil potentiating orthostatic hypotension caused by peripheral vasodilators.
Food Interaction
- Take with or without food. The absorption is unaffected by food.
Piloxidil Drug Interaction
Unknown: aspirin, aspirin, nebivolol, carvedilol, rosuvastatin, omega-3 polyunsaturated fatty acids, insulin glargine, furosemide, atorvastatin, metoprolol, metoprolol, esomeprazole, amlodipine, clopidogrel, pantoprazole, levothyroxine, acetaminophen, cyanocobalamin, ascorbic acid, cholecalciferol
Piloxidil Disease Interaction
Major: fluid retention/congestive heart failure, ischemic heart disease, pheochromocytomaModerate: renal failure/dialysis
Elimination Route
Piloxidil is at least 90% absorbed from the GI tract in experimental animals and man.
Half Life
4.2 hours
Pregnancy & Breastfeeding use
Piloxidil topical solution should not be used during pregnancy and lactation.
Contraindication
- Patients with cardiac abnormalities
- Children below 18 years of age
- Patients using occlusive dressings or other medicines on the scalp
- Patients with red, inflamed infection, or irritated or painful scalp (including psoriasis & sunburn)
Acute Overdose
Increased systemic absorption of Piloxidil may potentially occur if higher-than-recommended doses of Piloxidil are applied to larger surface areas of the body or areas other than the scalp. There are no known cases of Piloxidil overdosage resulting from topical administration of Piloxidil.
Signs and symptoms of Piloxidil overdosage would primarily be cardiovascular effects associated with sodium and water retention, and tachycardia. Fluid retention can be managed with appropriate diuretic therapy. Clinically significant tachycardia can be controlled by administration of a beta-adrenergic blocking agent.
Storage Condition
Store at a cool and dry place, protected from light. Keep out of the reach of the children.
Innovators Monograph
You find simplified version here Piloxidil
Piloxidil contains Minoxidil see full prescribing information from innovator Piloxidil Monograph, Piloxidil MSDS, Piloxidil FDA label
FAQ
What is Piloxidil used for?
Piloxidil is a medication used for the treatment of high blood pressure and pattern hair loss in males and females. Piloxidil applied to the scalp is used to stimulate hair growth in adult men and women with a certain type of baldness.
How safe is Piloxidil?
This over-the-counter product is considered safe, but should be used with caution. Furthermore, Piloxidil is an orally active vasodilator for treatment of severe hypertension.
How does Piloxidil work?
works by shortening the telogen phase of your hair growth cycle and moving your hairs into the anagen.
What are the common side effects of Piloxidil?
Common side effects of Piloxidil are include:
- Irritation
- Eczema
- Abnormal hair growth on the body
- Allergic contact dermatitis
- Application site redness
- Worsening of hair loss
- Burning
- Respiratory infections
- Tendinitis
- Back pain
- Fractures
- Sinusitis
- Fluid retention (edema)
- Anxiety
- Low blood pressure (hypotension)
- Dizziness
- Lightheadedness
- Faintness
Is Piloxidil safe during pregnancy?
It is not known whether Piloxidil topical will harm an unborn baby. Do not use this medicine without a doctor's advice if you are pregnant. Piloxidil should be used during pregnancy only if the possible benefit outweighs the possible risk to the unborn baby.
Is Piloxidil safe during breastfeeding?
Studies in women suggest that this medication poses minimal risk to the infant when used during breastfeeding.
Can I drink alcohol with Piloxidil?
Piloxidil does not significantly react with alcohol use. However, alcohol can dry out the skin, which could irritate your scalp when using topical Piloxidil products.
When should be taken of Piloxidil?
Piloxidil is a topical medication that you apply directly to your scalp. It's designed for use two times a day. Most people who use Piloxidil apply it once in the morning and once in the evening, typically a few hours before going to bed.
Can I take Piloxidil on an empty stomach?
Piloxidil may be taken with food or on an empty stomach.
How long can I take Piloxidil?
Most people need to use this medication regularly for 4 months to see benefit. This medication must be used continuously to maintain hair growth. If your condition does not improve or worsens after using this medication for 4 to 6 months.
Is Piloxidil bad for the heart?
Piloxidil can cause poor heart function or worsen existing heart problems.
How long does Piloxidil take to work?
Generally speaking, it takes about 8 weeks of consistent use to start to see results with Piloxidil. After 4 months of use, you should start to see the end of hair loss and start to see hair growth.
How long does Piloxidil stay in my system?
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 effect is approximately 75 hours.
What happens If I stop taking Piloxidil?
If you stop applying Piloxidil to your scalp, you'll gradually lose any hair that you've regrown as a result of the medication. Piloxidil is a well-studied medication that's safe to use for the long term.
Who should not take Piloxidil?
Do not use Piloxidil topical if the skin on your scalp is red, swollen, irritated, or infected.
What happens if I miss a dose?
Apply the missed dose as soon as you remember. Skip the missed dose if it is almost time for your next dose. Do not use extra medicine to make up the missed dose.
What happens if I overdose?
An overdose of Piloxidil topical is not expected to be dangerous. Seek emergency medical attention if anyone has accidentally swallowed the medication.
Can Piloxidil affects my heart ?
Piloxidil can cause poor heart function or worsen existing heart problems.
Can Piloxidil affect my kidneys?
If it continues for a long time, the heart and arteries may not function properly. This can damage the blood vessels of the brain, heart, and kidneys, resulting in a stroke, heart failure, or kidney failure.
Can Piloxidil affects my liver?
Piloxidil is metabolized by the liver, but has little effect on hepatic metabolism of other drugs. The reason for its lack of hepatotoxicity is not known.
Will Piloxidil affect my fertility?
There is accumulating evidence that it negatively impacts male fertility. You may instead use topical Piloxidil, which has no known negative effects on male fertility.
