Mechanism of action
Rentylin is a methylxanthine derivative and nonselective inhibitor of the cyclic nucleotide phosphodiesterases that increase the rate of breakdown of cAMP and cGMP. The drug has two major clinical effects:
increasing microvascular blood flow, thereby enhancing oxygenation of ischemic tissue. This effect is attributed to increased erythrocyte membrane deformability, vasodilation, reduced erythrocyte and platelet aggregation and enhanced fibrinolysis
immunomodulation, particularly by suppressing synthesis of proinflammatory cytokines (IL-1, IL-6, IL-12, TNF-a) by lymphocytes and keratinocytes and inhibiting adhesion between leukocytes and endothelial or epithelial cells. There may also be inhibitory effects on neutrophil, T and B lymphocytes and NK cell activity.
Formulations and dose rates
A range of dose rates is reported and long-term therapy is generally indicated with a trial period of 2–3 months
Rentylin has been administered to dogs with dermatomyositis or ulcerative dermatosis at 400 mg/dog q.12 h (or for small dogs 200 mg/dog q.12 h) and to dogs with contact dermatitis or atopic dermatitis at 10 mg/kg q.12 h PO. Combination prednisone and Rentylin therapy is reported for the management of cutaneous rabies vaccine-induced vasculitis in dogs. Rentylin is not a licensed veterinary medicine
Rentylin extended-release tablets, USP for oral administration contain 400 mg of the active drug and the following inactive ingredients: D&C Red No. 30 Aluminum Lake, FD&C Blue No. 2 Aluminum Lake, FD&C Yellow No. 6 Aluminum Lake, hydroxyethylcellulose, hypromellose, magnesium stearate, microcrystalline cellulose, polydextrose, polyethylene glycol, povidone, titanium dioxide and triacetin in an extended-release formulation. Rentylin extended-release tablets are a tri-substituted xanthine derivative designated chemically as 1-(5-oxohexyl)-3,7-dimethylxanthine that, unlike theophylline, is a hemorrheologic agent, i.e., an agent that affects blood viscosity. Rentylin is soluble in water and ethanol, and sparingly soluble in toluene. The CAS Registry Number is 6493-05-6.
The chemical structure is:
Rentylin may also be beneficial in other diseases such as Kimura's disease with oral ulcers, generalized granuloma annulare, sweet syndrome, pemphigus vulgaris and other bullous disorders.
Stevens-Johnson syndrome and toxic ep >Rentylin has been used as a miscellaneous drug for SJS and TEN, especially in children.
Is Trental safe to use during pregnancy or while breastfeeding?
Rentylin has not been adequately studied in pregnant women.
Rentylin is excreted in breast milk and may cause adverse effects in the infant.
Carcinogenesis, Mutagenesis and Impairment of Fertility
Long-term studies of the carcinogenic potential of Rentylin were conducted in mice and rats by dietary administration of the drug at doses up to 450 mg/kg (approximately 19 times the maximum recommended human daily dose (MRHD) in both species when based on body weight; 1.5 times the MRHD in the mouse and 3.3 times the MRHD in the rat when based on body surface area). In mice, the drug was administered for 18 months, whereas in rats, the drug was administered for 18 months followed by an additional 6 months without drug exposure. In the rat study, there was a statistically significant increase in benign mammary fibroadenomas in females of the 450 mg/kg group. The relevance of this finding to human use is uncertain. Rentylin was devo >Salmonella (Ames test) and in cultured mammalian cells (unscheduled DNA synthesis test) when tested in the presence and absence of metabolic activation. It was also negative in the in vivo mouse micronucleus test.
How is this medicine (Rentylin) best taken?
Use Rentylin as ordered by your doctor. Read all information given to you. Follow all instructions closely.
- Take with meals.
- Swallow tablet whole. Do not chew, break, or crush.
- To gain the most benefit, do not miss doses.
- Keep taking Rentylin as you have been told by your doctor or other health care provider, even if you feel well.
What do I do if I miss a dose?
- Take a missed dose as soon as you think about it, with a meal.
- If it is close to the time for your next dose, skip the missed dose and go back to your normal time.
- Do not take 2 doses at the same time or extra doses.
Rentylin extended-release tablets, USP for oral administration contain 400 mg of the active drug and the following inactive ingredients: colloidal silicon dioxide, hydroxypropyl cellulose, hypromellose, magnesium stearate, polyethylene glycol, and titanium dioxide in an extended-release formulation. Rentylin is a tri-substituted xanthine derivative designated chemically as 3,7- Dihydro-3,7-dimethyl-1-(5-oxohexyl)-1H-purine-2,6-dione that, unlike theophylline, is a hemorrheologic agent, i.e., an agent that affects blood viscosity. Rentylin is soluble in water and ethanol, and sparingly soluble in toluene. The molecular formula is C13H18N4O3 and its molecular weight is 278.31.
The chemical structure is:
USP Dissolution Test 9
Radiation induced fibrosis and burns
Radiation induced fibrosis is mediated by TGF-β, besides its central role in scleroderma. TGF-beta induced collagen biosynthesis is reduced by Rentylin. In addition, fibroblast collagenases are also activated. Hence, the treatment of radiation induced fibrosis with Rentylin and vitamin E can be a practicable and cost-effective regimen, especially for inoperable patients. Rentylin has been found to have a direct effect on inhibiting burn scar fibroblasts and it can be potentially useful for reducing burn scar contractures in future.