Hair Restore Ultra Scalp Solution

Minoxidil

Vasodilatory Effect: Minoxidil primarily acts as a direct vasodilator by relaxing arterial smooth muscle, which reduces peripheral resistance and lowers blood pressure. It does not affect the central nervous system or adrenergic neurons, and it maintains its activity even after adrenergic denervation.

Role of cAMP: Minoxidil may increase cyclic adenosine monophosphate (cAMP) levels by inhibiting phosphodiesterase, which contributes to its vasodilatory effects.

Compensatory Responses: Like other direct vasodilators, minoxidil causes a compensatory increase in heart rate, stroke volume, and plasma renin activity, leading to sodium and water retention. This compensatory mechanism may reduce its hypotensive effects, necessitating the use of a beta-blocker or diuretics to manage these responses.

Hair Growth: The exact mechanism for hair growth stimulation is unclear but is believed to be independent of its vasodilatory effects. Topical minoxidil accelerates the transition of hair follicles from the telogen (resting) phase to the anagen (growth) phase. It may also influence calcium dynamics and the metabolism of androgens in the scalp, although direct follicle formation has not been observed.

Azelaic Acid

Antimicrobial Activity: Azelaic acid inhibits microbial protein synthesis, exhibiting bacteriostatic and, at higher concentrations, bactericidal effects against acne-related bacteria such as Staphylococcus epidermidis and Propionibacterium acnes.

Anti-inflammatory and Antikeratinizing Effects: It reduces inflammation by scavenging oxygen radicals and normalizes keratinization in the follicle by decreasing filaggrin synthesis. This action helps reduce noninflamed acne lesions.

Other Effects: Azelaic acid may have antiproliferative actions, affecting oxidoreductive enzymes and causing changes in cellular lipid accumulation and mitochondrial function. Its effectiveness in conditions like melasma and malignant melanoma is related to reduced melanogenesis and altered melanocyte activity.

Finasteride

5-alpha-Reductase Inhibition: Finasteride is a specific inhibitor of type II 5-alpha-reductase, an enzyme responsible for converting testosterone to dihydrotestosterone (DHT). DHT is a potent androgen involved in prostate tissue development and androgenetic alopecia.

Prostate Health: By reducing DHT levels, finasteride decreases prostate size and improves urine flow in benign prostatic hyperplasia (BPH) patients.

Hair Loss: In male pattern baldness, finasteride lowers DHT concentrations in the scalp, helping to mitigate hair follicle miniaturization and promote hair regrowth. It does not significantly affect other hormone levels or the hypothalamic-pituitary-testicular axis.

Ketoconazole

Antifungal Action: Ketoconazole inhibits ergosterol synthesis by interacting with 14-alpha demethylase, an essential enzyme for fungal cell membrane integrity. This leads to increased cell membrane permeability and leakage of cellular contents.

Additional Mechanisms: Ketoconazole also affects human steroid synthesis, including aldosterone, cortisol, and testosterone. It can inhibit testosterone secretion at lower doses than cortisol. Its broad action on steroid synthesis and inhibition of thromboxane synthesis contribute to its use in treating advanced prostate cancer and other conditions.

Each component of the Hair Restore Ultra Scalp Solution targets different aspects of hair loss and scalp health, combining to offer a multifaceted approach to treatment.

Minoxidil

Contraindications:

Cardiac Disease: Minoxidil is contraindicated in patients with cardiac conditions like angina, coronary artery disease, recent myocardial infarction, or cerebrovascular disease due to the risk of exacerbating these conditions with reflex tachycardia and hypotension.

Renal Disease: Avoid in patients with severe renal failure (CrCl < 10 ml/min). Use cautiously in those with renal impairment as dosage adjustments may be needed.

Pheochromocytoma: Contraindicated due to the risk of stimulating catecholamine secretion.

Pulmonary Hypertension/CHF: Use with caution as it may increase pulmonary artery pressure and exacerbate these conditions.

Topical Use in Severe Skin Conditions: Avoid use on areas with skin abrasions or irritations (e.g., psoriasis, sunburn) due to increased systemic absorption risk.

Precautions:

Cardiac Monitoring: Minoxidil should be administered under close supervision, typically with a beta-blocker and diuretic to prevent reflex tachycardia and fluid retention.

Hospitalization: Initiate in a hospital setting for patients with malignant hypertension or those receiving guanethidine to monitor for orthostatic effects.

Elderly: Use cautiously; systemic dose selection should start at the lower end of the range due to potential decreased hepatic, renal, or cardiac function.

Azelaic Acid

Contraindications:

Propylene Glycol Hypersensitivity: Avoid formulations containing propylene glycol in patients with hypersensitivity to this ingredient.

Ocular and Mucosal Contact: Avoid contact with eyes and mucous membranes; if contact occurs, rinse thoroughly and consult a physician if irritation persists.

Herpes Labialis: Avoid application to areas affected by herpes labialis to prevent exacerbation.

Precautions:

Dark Complexions: Use cautiously in patients with darker skin tones due to the risk of hypopigmentation.

Pediatric Use: Safety and efficacy have not been established in children under 12 years for cream and gel formulations; foam is not approved for those under 18.

Asthma: Monitor for worsening of asthma symptoms and discontinue if exacerbation occurs.

Finasteride

Contraindications:

Pediatric Patients: Not indicated for use in individuals under 18 years of age.

Pregnant Women: Do not donate blood while on finasteride to prevent exposure to pregnant women due to potential teratogenic effects.

Precautions:

Hepatic Disease: Use with caution in patients with hepatic impairment as finasteride is metabolized in the liver.

PSA Levels: PSA levels may be significantly reduced; adjust values accordingly when interpreting PSA tests for prostate cancer detection.

Prostate Cancer Risk: Potential increased risk of high-grade prostate cancer; balance benefits against risks.

Infertility: May affect semen quality; consider potential impact on fertility.

Ketoconazole

Contraindications:

CYP3A4 Interactions: Avoid use with drugs metabolized by CYP3A4 due to the risk of elevated plasma concentrations and QT interval prolongation.

Oral Use in Children: Oral ketoconazole is not FDA-approved for neonates, infants, or children under 2 years.

Precautions:

Cardiac Conditions: Use with caution in patients with cardiac disease or conditions increasing QT interval risk.

Adrenal Insufficiency: Monitor for adrenal insufficiency, especially at doses ≥400 mg/day.

Hypersensitivity: Contraindicated in patients with known azole hypersensitivity.

Topical Use: Be cautious with topical formulations due to flammability and potential ocular exposure.

Minoxidil

Contraindications:

• Cardiac Disease: Minoxidil is contraindicated in patients with cardiac conditions like angina, coronary artery disease, recent myocardial infarction, or cerebrovascular disease due to the risk of exacerbating these conditions with reflex tachycardia and hypotension.
• Renal Disease: Avoid in patients with severe renal failure (CrCl < 10 ml/min). Use cautiously in those with renal impairment as dosage adjustments may be needed.
• Pheochromocytoma: Contraindicated due to the risk of stimulating catecholamine secretion.
• Pulmonary Hypertension/CHF: Use with caution as it may increase pulmonary artery pressure and exacerbate these conditions.
• Topical Use in Severe Skin Conditions: Avoid use on areas with skin abrasions or irritations (e.g., psoriasis, sunburn) due to increased systemic absorption risk.

Precautions:

• Cardiac Monitoring: Minoxidil should be administered under close supervision, typically with a beta-blocker and diuretic to prevent reflex tachycardia and fluid retention.
• Hospitalization: Initiate in a hospital setting for patients with malignant hypertension or those receiving guanethidine to monitor for orthostatic effects.
• Elderly: Use cautiously; systemic dose selection should start at the lower end of the range due to potential decreased hepatic, renal, or cardiac function.

Azelaic Acid

Contraindications:

• Propylene Glycol Hypersensitivity: Avoid formulations containing propylene glycol in patients with hypersensitivity to this ingredient.
• Ocular and Mucosal Contact: Avoid contact with eyes and mucous membranes; if contact occurs, rinse thoroughly and consult a physician if irritation persists.
• Herpes Labialis: Avoid application to areas affected by herpes labialis to prevent exacerbation.

Precautions:

• Dark Complexions: Use cautiously in patients with darker skin tones due to the risk of hypopigmentation.
• Pediatric Use: Safety and efficacy have not been established in children under 12 years for cream and gel formulations; foam is not approved for those under 18.
• Asthma: Monitor for worsening of asthma symptoms and discontinue if exacerbation occurs.

Finasteride

Contraindications:

Pediatric Patients: Not indicated for use in individuals under 18 years of age.

Pregnant Women: Do not donate blood while on finasteride to prevent exposure to pregnant women due to potential teratogenic effects.

Precautions:

Hepatic Disease: Use with caution in patients with hepatic impairment as finasteride is metabolized in the liver.

PSA Levels: PSA levels may be significantly reduced; adjust values accordingly when interpreting PSA tests for prostate cancer detection.

Prostate Cancer Risk: Potential increased risk of high-grade prostate cancer; balance benefits against risks.

Infertility: May affect semen quality; consider potential impact on fertility.

Ketoconazole

Contraindications:

CYP3A4 Interactions: Avoid use with drugs metabolized by CYP3A4 due to the risk of elevated plasma concentrations and QT interval prolongation.

Oral Use in Children: Oral ketoconazole is not FDA-approved for neonates, infants, or children under 2 years.

Precautions:

Cardiac Conditions: Use with caution in patients with cardiac disease or conditions increasing QT interval risk.

Adrenal Insufficiency: Monitor for adrenal insufficiency, especially at doses ≥400 mg/day.

Hypersensitivity: Contraindicated in patients with known azole hypersensitivity.

Topical Use: Be cautious with topical formulations due to flammability and potential ocular exposure.

Adverse Reactions / Side Effects

Minoxidil

Topical Use:

Dermatological Reactions: Includes contact dermatitis, local burning, pruritus, erythema, and xerosis.

Hypertrichosis: Elongation and thickening of fine body hair, which can occur on the temples, between the eyebrows, or in the sideburn area. Reversible upon discontinuation.

Local Reactions: Rarely includes bullous rash and Stevens-Johnson syndrome.

Gastrointestinal Effects: Nausea and vomiting may occur with oral minoxidil.

Oral Use:

Fluid Retention: Includes edema and ascites; often requires concomitant diuretic use.

Reflex Tachycardia: May lead to headache, angina, and increased myocardial oxygen demand.

Hematologic Effects: Temporary reductions in hematocrit, hemoglobin, and erythrocyte count; increases in serum creatinine and BUN; potential thrombocytopenia and leukopenia.

Hypertrichosis: Can affect various body areas.

Azelaic Acid

Dermatologic Reactions: Burning sensation, paresthesias, pruritus, xerosis, erythema, skin irritation, contact dermatitis, rash, peeling, dermatitis, and edema.

Pigmentation Changes: Potential hypopigmentation in dark-skinned patients.

Rare Reactions: Vitiligo, hypertrichosis, reddening, and exacerbation of herpes labialis.

Post-marketing Reports: Includes hypersensitivity reactions (angioedema, ocular inflammation, facial swelling, urticaria), asthma exacerbation, and iridocyclitis.

Finasteride

Sexual Dysfunction: Includes impotence (erectile dysfunction), decreased libido, decreased ejaculate volume, ejaculation dysfunction, and breast tenderness.

Gynecomastia: Reported in a significant number of patients; often resolves after discontinuation, but rare cases of breast cancer have been noted.

Infertility Effects: Reduced sperm count, decreased sperm motility, and decreased semen volume; normalization or improvement may occur after discontinuation.

Teratogenic Effects: Potential for abnormalities in the external genitalia of the male fetus.

Ketoconazole

Gastrointestinal Effects: Nausea, vomiting, abdominal pain, and diarrhea.

Dermatologic Reactions: Includes cheilitis, pruritus, alopecia, skin irritation, contact dermatitis, and xerosis.

Hormonal Effects: Can inhibit testosterone and cortisol synthesis, leading to gynecomastia, impotence, and oligospermia.

Systemic Reactions: Rare cases of anaphylactoid reactions, hypersensitivity reactions, fever, chills, dizziness, drowsiness, and photophobia.

Ophthalmic Effects: Includes ocular irritation and keratoconjunctivitis sicca.

Cardiovascular Effects: QT prolongation, ventricular arrhythmias, and torsade de pointes, especially with other QT-prolonging drugs.

Vitamin D Deficiency: May require monitoring and supplementation.

Minoxidil

Pregnancy:

• Risk Category: C
• Effects: Animal studies show adverse effects, including reduced fertility and survival of offspring. Dysmorphic facial features and hypertrichosis were observed in an infant whose mother took 10 mg daily during pregnancy.
• Guidance: Should be used only if the benefits outweigh the risks.

Breastfeeding:

• General Guidance: Minoxidil is generally considered compatible with breastfeeding by the American Academy of Pediatrics (AAP), but some experts are cautious.
• Effects: Minoxidil is excreted into breast milk, but the impact of prolonged exposure is unknown. Alternative antihypertensives with more safety data include enalapril, hydrochlorothiazide, methyldopa, and propranolol.

Azelaic Acid

Pregnancy:

• Risk Category: B
• Effects: Animal data show embryotoxicity with oral administration but no teratogenic effects. No well-controlled studies in pregnant women.
• Guidance: Use only if clearly needed due to lack of comprehensive human data.

Breastfeeding:

• General Guidance: Caution is advised. Azelaic acid may be distributed into breast milk, but systemic absorption from topical use is low (<4%). The risk to the breastfeeding infant is considered minimal.

Finasteride

Pregnancy:

• Risk Category: Not FDA-approved for females of childbearing potential.
• Effects: Can cause fetal harm, including abnormalities in male external genitalia due to inhibition of testosterone conversion. Pregnant women or those trying to conceive should avoid handling crushed or broken tablets.
• Guidance: Strictly contraindicated during pregnancy.

Breastfeeding:

• General Guidance: Not FDA-approved for use in breastfeeding. The excretion of finasteride in human milk is unknown, and the effects on a nursing infant are not determined.

Ketoconazole

Pregnancy:

• Risk Category: No adequate studies in human pregnancy.
• Effects: Animal studies show embryotoxic and teratogenic effects at high doses. Guidelines recommend avoiding oral azole antifungals during pregnancy.
• Guidance: Use only if the benefits justify the risks.

Breastfeeding:

• Systemic Use: Excreted in breast milk, but at low concentrations. A breastfeeding infant’s exposure is minimal (0.4% of the maternal dose).
• Topical Use: Likely low concentrations in milk, but avoid applying directly to the nipple and areola.
• Guidance: Refrain from breastfeeding during oral ketoconazole therapy; consider alternatives like fluconazole if necessary.

Store this medication in its original container at 68°F to 77°F (20°C to 25°C) and away from heat, moisture and light. Keep all medicine out of the reach of children. Throw away any unused medicine after the beyond use date. Do not flush unused medications or pour down a sink or drain