Anti-Aging Vita Gel

Tretinoin (All-Trans-Retinoic Acid)

• Mechanism: Tretinoin, a retinoid, regulates cell differentiation, proliferation, and apoptosis through nuclear receptors. It binds to Retinoic Acid Receptors (RARs) and has minimal interaction with Retinoid X Receptors (RXRs).
  • RARs: Tretinoin binds to all three RAR types—RAR-alpha, RAR-beta, and RAR-gamma—each having different effects on the body. For example:
    • RAR-alpha: Involved in the differentiation of acute promyelocytic leukemia (APL) cells.
    • RAR-beta: Associated with squamous cell carcinomas.
    • RAR-gamma: Influences mucocutaneous tissues and bone.
• Skin Disorders: Tretinoin accelerates cell turnover, reduces cell cohesion, and prevents comedone formation. It modifies gene expression and protein synthesis, leading to improved epithelial cell growth and differentiation.
• Photodamage: It inhibits the activity of matrix metalloproteinases (MMPs) induced by UV irradiation, reducing collagen degradation and mitigating signs of photodamage like wrinkling and hyperpigmentation.
• Acute Promyelocytic Leukemia (APL): Tretinoin induces differentiation of APL cells by converting the inhibitory effects of the PML-RAR-alpha fusion protein to stimulatory effects, aiding in the treatment of this leukemia.

Niacinamide (Vitamin B3)

• Mechanism: Niacinamide, the amide form of niacin, is involved in the synthesis of NAD and NADP, crucial coenzymes in redox reactions. It participates in cellular metabolic pathways and energy production.
  • Redox Reactions: NAD and NADP play roles in converting fats and proteins into glucose and in the oxidation of glucose.
• Pharmacologic Effects:
  • Nicotinic Acid (Niacin): Acts as an antilipemic by reducing total serum cholesterol, LDL, VLDL, and triglycerides, while increasing HDL. The mechanism includes decreased hepatic VLDL synthesis and various other effects on lipolysis and lipid metabolism.
  • Nicotinamide: Unlike nicotinic acid, it does not induce flushing and lacks hypolipidemic effects. It is primarily used in skincare for its anti-inflammatory properties and to improve skin barrier function.

Vitamin C

• Absorption: Vitamin C is absorbed through both simple diffusion and active transport mechanisms involving hexose transporters and sodium-dependent vitamin C transporters (SVCTs). It is primarily absorbed in the distal small intestine.
• Functions:
  • As a Cofactor: Vitamin C acts as a cofactor in several enzyme reactions, including those involved in collagen synthesis and metabolism of carnitine and catecholamines.
  • Antioxidant: It neutralizes free radicals and reduces oxidative stress.
  • Iron Absorption: Enhances the absorption of dietary iron.
  • Other Effects: Stabilizes vitamin E and folic acid, and modulates inflammatory responses, contributing to overall cellular health and immune function.

These mechanisms highlight how each compound works at a cellular level to contribute to skin health, cellular function, and overall well-being.

Tretinoin

• Contraindications:
  • Hypersensitivity: Contraindicated in patients with a known hypersensitivity to vitamin A or other retinoids due to the possibility of cross-sensitivity.
  • Fish Protein Allergy: Brands like Atralin and Altreno contain fish proteins and should be used cautiously in those with fish allergies.
  • Eczema: Should be avoided in patients with eczema due to the risk of severe irritation.
  • Neonates and Infants: Safety and efficacy in children under 12 years have not been established except for specific formulations.
• Precautions:
  • Acute Promyelocytic Leukemia (APL): Monitor for retinoic acid-APL syndrome, characterized by rapidly increasing leukocyte counts and differentiation syndrome.
  • Photosensitivity: Use sunscreen and avoid excessive sun exposure to prevent increased irritation.
  • Sunburn: Avoid use on sunburned skin until it has healed.
  • Pregnancy: Not established in neonates and should be used with caution in pregnant women; may cause severe headache and pseudotumor cerebri in children.
  • Application Areas: Avoid contact with eyes, mouth, and mucous membranes. Tretinoin is flammable, so avoid use near heat or open flames.

Niacinamide

• Contraindications:
  • Hypersensitivity: Contraindicated in those with known hypersensitivity to niacin or its components.
  • Hepatic Disease: Avoid in patients with significant hepatic disease or those with a history of hepatic dysfunction.
  • Peptic Ulcer Disease: Contraindicated in active peptic ulcer disease due to its potential to exacerbate symptoms.
• Precautions:
  • Liver Monitoring: Monitor liver function tests regularly, especially with extended-release formulations.
  • Hypotension and Cardiovascular Issues: Use cautiously in patients with hypotension, acute myocardial infarction, or unstable angina.
  • Diabetes: Monitor blood sugar levels as niacin can cause hyperglycemia.
  • Gout: Caution in patients with gout as it may cause hyperuricemia.
  • Renal Disease: Use with caution in patients with renal impairment.
  • Pregnancy and Breastfeeding: Generally safe in recommended daily allowances, but high doses should be avoided. Monitor for adverse effects in breastfeeding infants.

Vitamin C

• Contraindications:
  • Blood Conditions: Avoid in patients with thalassemia, G6PD deficiency, sickle cell disease, and hemochromatosis.
  • Nephrolithiasis: Use cautiously in patients with oxalate nephropathy or nephrolithiasis.
• Precautions:
  • Diabetes: Caution with diabetes as it may elevate blood sugar levels.
  • Angioplasty: Avoid taking supplements right before or after angioplasty.

Vitamin E

• Contraindications:
  • High Doses: High doses can increase bleeding risk due to vitamin K antagonism.
• Precautions:
  • Pregnancy: Use high doses cautiously; normal intake levels are generally safe.
  • Breastfeeding: Generally safe at recommended doses, but avoid excessive topical application.
  • Premature Infants: Monitor serum levels carefully to avoid complications like sepsis and necrotizing enterocolitis.

Tretinoin

• Topical Use:
  • Common Side Effects: Peeling, dry skin (xerosis), burning, stinging, redness (erythema), itching (pruritus).
  • Severe Reactions: Severe irritation leading to temporary discontinuation or use of corticosteroids (7% of patients), skin hyperpigmentation or hypopigmentation (2% of patients), and severe local reactions such as erythema, edema, vesicles, or crusting may require discontinuation and less frequent application.
  • Photosensitivity: Increased sensitivity to sunlight; sunscreen and protective clothing are recommended.
  • Discontinuation Rate: About 4% due to adverse reactions.
  • Oral Use: Dry skin/mucous membranes (77%), rash (54%), itching (20%), alopecia (14%), and rare cases of erythema nodosum and Sweet’s syndrome.

Niacinamide

• General:
  • Common Side Effects: Flushing, warmth, burning or tingling of skin, especially in face, neck, and chest.
  • Gastrointestinal: Nausea, vomiting, abdominal pain, diarrhea, bloating, dyspepsia, and flatulence. More common with high doses.
  • Liver: Jaundice, elevated hepatic enzymes, risk of hepatic necrosis with sustained-release products. Regular liver function tests are advised.
  • Glucose Metabolism: Hyperglycemia and exacerbation of diabetes, especially with high doses.
  • Uric Acid: Hyperuricemia and gout in some patients.
  • Electrolytes: Hypophosphatemia and occasional decreases in platelet counts or increased prothrombin times.
  • Other: Asthenia, nervousness, insomnia, paresthesias, and rare cases of rhabdomyolysis. Ophthalmic effects like blurred vision and macular edema.

Vitamin E Acetate

• General:
  • High Doses in Adults: Risk of bleeding complications, breast enlargement, fatigue, intestinal cramps, weakness, blurred vision, headache, gonadal dysfunction, increased serum cholesterol and triglycerides.
  • In Premature Infants: Risk of necrotizing enterocolitis, infections, or sepsis. Monitor serum concentrations closely.
  • Topical Use: Contact dermatitis and other rashes.

Vitamin C

• General:
  • Common Side Effects: Nausea, diarrhea, and abdominal cramps. High doses may cause lower back pain. Consult a doctor if severe side effects occur.

Tretinoin

• Pregnancy – Topical Use: Adequate studies are lacking, but significant risks are known from other retinoids, including birth defects. Avoid large-area or prolonged use. The benefit-risk profile should be assessed, and reproductive risks discussed.
• Pregnancy – Oral Use: High risk of birth defects. Females of childbearing potential must use two reliable forms of contraception during therapy and for one month afterward. Pregnancy tests should be done before and during therapy.
• Breastfeeding – Topical Use: Systemic absorption is low, so significant transfer into breast milk is unlikely. However, alternative topical agents may be considered.
• Breastfeeding – Oral Use: Breastfeeding should be discontinued. The drug’s transfer into milk is unknown.

Niacinamide

• Pregnancy – Recommended Daily Allowance (RDA): Considered safe and classified as pregnancy category A.
• Pregnancy – High Doses: Categorized as pregnancy category C. Use high doses with caution, and only if the benefits outweigh the risks.
• Breastfeeding – General: Excretion into breast milk is expected. Manufacturers recommend discontinuing nursing or the drug if adverse effects occur in infants. The RDA for lactating women is 20 mg.

Vitamin C

• Pregnancy – RDA: Classified as pregnancy category A and generally considered safe.
• Pregnancy – High Doses: Pregnancy category C. Use only if benefits outweigh risks.
• Breastfeeding – General: Ascorbic acid is present in breast milk. Exercise caution with high doses.

Vitamin E Acetate

• Pregnancy – RDA: Generally safe. Excessive amounts should be avoided unless specifically needed.
• Breastfeeding – General: Vitamin E is transferred into breast milk but less than through the placenta. The use of vitamin E supplements should be cautious and generally limited to the RDA.

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.