Диферелин

Диферелин Uses, Dosage, Side Effects, Food Interaction and all others data.

Диферелин is a synthetic decapeptide agonist analog of luteinizing hormone releasing hormone (LHRH). Possessing greater potency than endogenous LHRH, triptorelin reversibly represses gonadotropin secretion. After chronic, continuous administration, this agent effects sustained decreases in LH and FSH production and testicular and ovarian steroidogenesis. Serum testosterone concentrations may fall to levels typically observed in surgically castrated men.

The first administration of triptorelin is followed by a transient surge of follicle stimulating hormone (FSH), luteinizing hormone (LH), estradiol,and testosterone. The time, peak and decline of testosterone in the body varies depending on the dose administered. This initial surge is often responsible for worsening of prostate cancer symptoms such as urethral or bladder outlet obstruction, bone pain, spinal cord injury and hematuria in the early stages. A sustained decrease in FSH and LH, and significant reduction of testicular steroidogenesis is usually seen 2-4 weeks post-initiation of therapy. This result is a reduction of serum testosterone to levels which are typically seen in surgically castrated men. Ultimately, tissues and functions that require these hormones become inactive. The effects of triptorelin can usually be reversed once the drug is discontinued.

Диферелин
Uses
Dosage
Side Effect
Precautions
Interactions
Uses during Pregnancy
Uses during Breastfeeding
Accute Overdose
Food Interaction
Half Life
Volume of Distribution
Clearance
Interaction With other Medicine
Contradiction
Storage

Trade Name	Диферелин
Availability	Prescription only
Generic	Triptorelin
Triptorelin Other Names	Triptorelin, Triptorelina, Triptoreline, Triptorelinum
Related Drugs	Triptodur, Supprelin LA, estradiol, tamoxifen, Premarin, Lupron, Xtandi, leuprolide, Casodex, Zytiga
Type
Formula	C₆₄H₈₂N₁₈O₁₃
Weight	Average: 1311.473 Monoisotopic: 1310.630874772
Protein binding	Triptorelin does not bind to plasma proteins at clinically relevant concentrations.
Groups	Approved, Vet approved
Therapeutic Class
Manufacturer
Available Country	Russia, Ukraine
Last Updated:	September 19, 2023 at 7:00 am

Uses

Диферелин is a GnRH agonist indicated for the palliative treatment of advanced prostate cancer.

Диферелин is indicated for the palliative treatment of advanced prostate cancer.

Диферелин is also used to associated treatment for these conditions: Advanced Prostate Cancer, Controlled ovarian hyperstimulation therapy

How Диферелин works

Диферелин is a synthetic agonist analog of gonadotropin releasing hormone (GnRH). Animal studies comparing triptorelin to native GnRH found that triptorelin had 13 fold higher releasing activity for luteinizing hormone, and 21-fold higher releasing activity for follicle-stimulating hormone.

Toxicity

Some of the most commonly reported adverse effects of triptorelin are hot flushes reported in 58.6% of patients, skeletal pain in 12.1%, impotence in 7.1%, and headache in 5.0%. Other reported adverse effects include injection site pain, general body pain, leg pain, fatigue, hypertension, dizziness, diarrhea, vomiting, insomnia, emotional lability, anemia, pruritus, urinary tract infections, and urinary retention. Диферелин is classified as Pregnancy Category X and contraindicated in pregnant women or in women who may become pregnant. Hormonal changes caused by triptorelin increase the risk for pregnancy loss. Studies done on pregnant rats demonstrated maternal toxicity and embryo-fetal toxicities.

Food Interaction

No interactions found.

Диферелин Drug Interaction

Moderate: doxorubicin, tramadolMinor: sulfamethoxazole / trimethoprimUnknown: 5-hydroxytryptophan, paclitaxel protein-bound, aspirin, acetaminophen / dextromethorphan / guaifenesin / phenylephrine, contained in alcoholic beverages , ocular lubricant ophthalmic, aspirin, aspirin, ethanol, omega-3 polyunsaturated fatty acids, acetaminophen, levothyroxine, valproic acid, thiamine, cyanocobalamin, cholecalciferol, goserelin

Диферелин Disease Interaction

Moderate: cardiovascular disease, diabetes, QT prolongation, renal/liver dysfunction

Volume of Distribution

After a single IV dose of 0.5mg, the volume of distribution of triptorelin peptide in healthy males was 30 - 33L.

Elimination Route

Following IV administration of triptorelin, triptorelin is completely absorbed.

Half Life

The pharmacokinetics of triptorelin follows a 3 compartment model. The half lives are estimated to be 6 minutes, 45 minutes, and 3 hours respectively.