【Description】

 

Milk white or pale yellow columniform suppositories. Main component of KAYUN is carboprost methylate suppositories, which chemical name is racemization (5Z,9α,11α,13E,15S)-9,11,15-trihyhydroxy-15-methyl prostaglandin-5,13-diene-1- acid methyl esters.

 

Structured Abstract: 

 

Molecular Formula：C₂₂H₃₈O₅ Molecular Weight: 382.54

 

【Pharmacology and toxicology】

 

KAYUN acts on uterine smooth muscle and has the function of antagonizing early pregnancy.

KAYUN has the excitatory function on the isolated uterus of rat and eutopic uterus of anaesthetic rabbit. KAYUN has significant antagonizing early pregnancy by vagina or subcutaneous administrating, and has synergetic effect combining with testasterone propionate and compound diphenoxylate tablet.

 

【Toxicology Action】

 

Acute toxicity: The LD50 of the female mouse administrated by subcutaneous injection is17.8±1.8 mg/kg.

 

The animal experiments indicate that subcutaneous injecting significant dose carboprost methylate has restraining effect on nerve system of level-headed mouse. This product has insignificant effect on blood pressure, electrocardiogram and rhythm of heart of the anaesthetic dog. Subcutaneous injecting for healthy monkey 0.1mg/kg of this product for 5 days continuously, or administrated 3 days with the dose of 0.1, 0.2, 0.3 mg/kg, significant effect on hemogram and the function of liver and kidney was not found. Study on the toxicity of local medication indicates that it will not stimulate and hurt the mucous membrane of the dog, administrated 1mg of this product by vagina. Ames experimentation indicates that it has no mutagenicity.

 

Observation of chromosome aberrance: General administration will not result in chromosome aberrance of the early pregnancy women.

 

【Pharmacokinetics】

It will absorb and metabolize quickly after administrating. The serum half life is around 30 minutes when it is administrated through vein and muscle, and the serum concentration will decrease quickly to the level that will not effect on the body after withdrawal. Administrating in dose form of suppository can reach the action position directly, meanwhile some are absorbed through vagina mucous membranes into circulatory system, but the serum concentration is hard to detect, and it will be excreted mainly through emiction 6~9 hours after administrating.

 

【Indication】

 

KAYUN (Carboprost Methylate) is used as terminating pregnancy medicine combined with Mifepristone subsequently for the treatment of early pregnancy, especially suitable for the high risk pregnant women, such as the women with several times artificial abortion, uterus abnormality, caesarean birth and the women in lactation period.

 

KAYUN is also indicated for preventing and curing postpartum hemorrhage caused by retarded uterine contraction.

 

【Dosage and Administration】

 

For terminating pregnancy of the healthy early pregnant women whose amenorrhea≤49,  taking 200mg of mifepristone tablet orally 2 hours before or after meals,  in the morning of the third day put one methyl carprost suppository (1mg) in the vagina posterior fornix . Or taking 50mg of mifepriston tablets in the morning and 25mg of mifepriston tablets at every 12 hours interval subsequently, in the morning of the third day, 1 hour after taking 25 mg of mifepriston tablets, putting one methyl carprost  suppository (1mg) in the vagina posterior fornix . Resting in the bed for 2 hours and clinically observing for 6 hours. Taking notice of condition of bleeding, removal of pregnancy substances and adverse reaction.

 

For postpartum hemorrhage, putting methyl carboprost suppository (1 mg) into the vagina, closed to the 1/3 below anterior wall of vagina for about 2 minutes.

 

【Contraindications】:

 

Do not be used for the patients with placenta previa, ectopic pregnancy, acute pelvic inflammation, gastric ulcer, asthma, serious atopy and glaucoma.

Be used cautiously for the patients with diabetes, high blood pressure, serious cardiac and renal insufficiency, hypohepatia.

 

【Precautions and warnings】

 

1. It should be used under the monitoring of the physician. Stop taking the drug when intolerable vomiting, abdominal pain or hemorrhage of vagina occurs.

 

2. The sterile glove should be used to put the drug into the vagina to prevent the secondary infection. 

 

3. For terminating early pregnancy, the drug should be combined with other drug, but not used solely.

 

4. Cautioned for the patients with diabetes, hypertension, serious heart, liver and renal insufficiency. 

 

【Adverse reactions】

 

Mainly they are diarrhea, queasiness or vomit, and bellyache etc. After taking compound diphenoxylate tablet, the adverse reactions will significant decrease. And these reactions will disappear after withdrawal.

 

【Interactions】

 

 Not known. Please consult your doctors before combined use with other drugs.

 

【Overdoses】

 

There have been no reports of toxicity from Carboprost Methylate overdosage. The LD50 of subcutaneous injection in mice is17.8±1.8 mg/kg. Large doses of Carboprost Methylate may cause inhibition of nervous system and influence blood pressure, electrocardiogram and rhythm.

 

【Strength】

 

0.5 mg; 1.0 mg

 

【Storage】

 

Preserve in tightly closed containers and cold (＜-5℃) place. Protect from light. 

 

【Package】

 

Packing material: polystyrene.

Packing specification: 5 suppositories/box

 

【Shelf life】

 

24 months

 

 

 

1. The derivative of prostaglandin F2α, safe and reliable.

 

2. Act directly to the target organ, and absorbed into the blood to avoid the first-pass effect.

 

3. Rapid onset and long period of action. It will take effect in about 5 minutes, have the most significant effect in 10-20 minutes, and last 60 min to maintain uterine contraction.

 

4. High pharmacoeconomics. It will give doctors and patients dual protection.

 

1. Caremery is indicated for preventing postpartum hemorrhage caused by uterine inertia.

 

Group 1: 130 cases, rectal administration of KAYUN with 1 mg; Group 2: 130 cases,vaginal administration of Caremery with 1 mg; Group 3: 50 cases, intramuscularly administrated Oxytocin 50 IU; Group 4: 50 cases, intravenously administrated Oxytocin 50 IU

 

 

Conclusion

 

Caremery has stronger uterine contraction than oxytocin. Caremery of 1 mg can significantly shorten the third labor stage, and reduce blood loss within 2 hours postpartum.

 

2. Caremery is indicated for promotion of postpartum uterine involution and intestinal exhaust.

 

Observation group: 50 cases, intravenously administrated Oxytocin 20 IU/d, rectally administrated Caremery 1 mg/12 h, 3 days.

Control group: 50 cases, intravenously administrated Oxytocin 20 IU/d, 3 days.

 

 Conclusion

 

Caremery has a significant effect on promoting uterine involution and recovery of the gastrointestinal tract after postpartum administration.

 

3. Caremery is indicated for treating postoperative urinary retention.

 

Caremery group: 16 cases, vaginally administrated 1 g/d for 5 days, interval of two days, cycle administration.

Conventional treatment group: 19 cases.

 

 

Conclusion

 

The average recovery period of Caremery group and Conventional treatment group are 13.1 days and 18.97 days, respectively.

 

 

 

Caremery is used for urination disorders after radical correction of cervical cancer, and consequently shorten the urinary retention time and reduce urethral injury and urinary tract infection.