Minoxidil, Piperidinyl Pyrimidinediamine Oxide, 38304-91-5

MINOXIDIL

Minoxidil / 6-(1-Piperidinyl)-2,4-pyrimidinediamine 3-oxide
CAS Number: 38304-91-5
EC Number: 254-484-5

SECTION 1: PRODUCT IDENTIFICATION AND CHEMICAL IDENTITY

Minoxidil is a synthetic pyrimidine derivative originally developed as an oral vasodilator for the treatment of hypertension. Its unexpected side effect of hypertrichosis (excessive hair growth) led to its development as a topical treatment for androgenetic alopecia (male and female pattern hair loss). It is the most widely used topical agent for hair loss treatment worldwide and is available in topical solution and foam formulations.

SECTION 2: SYNONYMS AND OTHER NAMES

SECTION 3: CHEMICAL STRUCTURE

3.1. Molecular Structure

Minoxidil is a pyrimidine derivative containing a piperidine ring attached to the pyrimidine core. The molecule contains an N-oxide functional group, which is responsible for its vasodilatory activity.

Structural Formula:

        NH₂
         |
         C
        / \
       /   \
      /     \
     /       \
    N         C
    |         |
    C - O⁻    C - NH₂
    |         |
    N         C
     \       /
      \     /
       \   /
        \ /
         N
         |
         C - N
        / \
       /   \
      /     \
     C       C
    / \     / \
   /   \   /   \
  H     H H     H
   \   /   \   /
    \ /     \ /
     C       C
      \     /
       \   /
        \ /
         H

Simplified Representation:

    NH₂
     |
     C
    / \
   /   \
  N     C
  |     |
  C=O   C-NH₂
  |     |
  N     C
   \   /
    \ /
     N
     |
     C - N
    / \
   /   \
  C     C
 / \   / \
H   H H   H
 \ /   \ /
  C     C
   \   /
    \ /
     H

3.2. Molecular Formula

C₉H₁₅N₅O

3.3. Molecular Weight

209.25 g/mol

3.4. Key Structural Features

SECTION 4: PHYSICAL AND CHEMICAL PROPERTIES

SECTION 5: SOLUBILITY PROFILE

SECTION 6: CHEMICAL PROPERTIES AND REACTIVITY

SECTION 7: PHARMACOLOGICAL PROPERTIES

7.1. Primary Mechanism of Action

7.2. Secondary Effects

SECTION 8: PHARMACOKINETICS

SECTION 9: APPLICATIONS AND INDUSTRIAL USES

9.1. Pharmaceutical and Medical Applications

9.2. Cosmetic Applications

9.3. Combination Products

SECTION 10: FORMULATION CONSIDERATIONS

SECTION 11: TOXICOLOGICAL PROFILE

SECTION 12: GHS CLASSIFICATION AND LABELING

Signal Word: WARNING

Hazard Pictograms: GHS07 (Exclamation Mark)

Hazard Statements (H-Codes):

SECTION 13: PRECAUTIONARY STATEMENTS (P-CODES)

SECTION 14: FIRST AID MEASURES

SECTION 15: FIRE-FIGHTING MEASURES

SECTION 16: ACCIDENTAL RELEASE MEASURES

SECTION 17: STORAGE AND SHELF LIFE

SECTION 18: PACKAGING OPTIONS

SECTION 19: TRANSPORT INFORMATION

SECTION 20: REGULATORY INFORMATION

SECTION 21: RELATED COMPOUNDS AND DERIVATIVES

SECTION 22: QUICK REFERENCE TABLE

SECTION 23: CRITICAL NOTICES AND BEST PRACTICES

CRITICAL NOTICES:

1. Toxicity: Minoxidil has moderate to high oral toxicity (LD50 ~120 mg/kg). Handle with care to prevent accidental ingestion.

2. Topical Use Only: For hair loss treatment, minoxidil is intended for topical use only. Oral use is for hypertension treatment and requires medical supervision.

3. Patient Counseling: Patients should be advised that hair growth may take 3-6 months of consistent use. Discontinuation leads to loss of newly grown hair within 3-6 months.

4. Skin Irritation: May cause local irritation (itching, redness, scaling, dermatitis). Patients with sensitive skin should start with lower concentrations (2%).

5. Systemic Absorption: Although minimal (approximately 1.4%), systemic absorption can occur, particularly with large-area application or damaged skin.

6. Pregnancy and Lactation: Use during pregnancy and lactation should be avoided unless clearly needed.

7. Storage: Protect from light and moisture. Store in tightly closed containers in a cool, dry place.

8. Formulation: For cosmetic formulations, ensure compatibility with other ingredients and appropriate preservative systems.

BEST PRACTICE RECOMMENDATIONS:

• Formulation: Use co-solvents such as propylene glycol and ethanol to enhance solubility. Consider using antioxidants to prevent oxidation.

• Packaging: Use light-resistant, moisture-protective packaging (aluminum foil bags, amber glass or opaque HDPE containers).

• Quality Control: Perform HPLC analysis for content uniformity and impurity profiling. Test for heavy metals and residual solvents.

• Patient Advice: Advise patients to apply to a dry scalp, massage gently, and wash hands after application. Consistent use is essential.

• Combination Therapy: May be combined with finasteride (oral) or ketoconazole shampoo for enhanced results.

LEGAL DISCLAIMER:

This Technical Data Sheet (TDS) is for informational purposes only and is prepared based on available technical data. The user is solely responsible for determining the suitability of the product for their specific application and for complying with all local, national, and international regulations. For complete safety, storage, handling, transport, waste, and regulatory compliance information, the official Safety Data Sheet (SDS/MSDS) provided by the manufacturer/supplier must be consulted. This document does not substitute professional or medical advice.