Trade Name: Cytotec, Misoprostol
Manufacturer: pfizer Pharma
Usage Application: ungewollte Schwangerschaft
Service Country: Germany France USA UK and europe
What is cytotec?
Cytotec is the brand name of misoprostol, a synthetic prostaglandin. and Cytotec, scientifically known as misoprostol, is a synthetic prostaglandin meticulously designed to shield the stomach from ulcers. It steps into action when aspirin or non-steroidal anti-inflammatory drugs (NSAIDs) are used to alleviate pain, combat fever, manage arthritis, or tackle inflammatory conditions.
This remarkable medication is available in a generic form, making it accessible to a broader spectrum of individuals. Whether you're seeking relief from stomach ulcers or considering its application in early pregnancy termination, Cytotec, in the form of Misoprostol 200mcg Tablets, offers a multifaceted solution. Learn more about its diverse applications and mechanisms in our comprehensive guide.
Cytotec Information 2023
n a study involving 4500 ulcer patients aged 60 or older, Cytotec displayed a safety profile comparable to that in younger patients. Furthermore, adverse events reported during clinical trials showed low incidence rates, with nausea (3.1%), flatulence (2.9%), headache (2.3%), dyspepsia (2.1%), vomiting (1.4%), and constipation (1.1%) being the most common. Notably, these adverse reactions were reported in more than 1% of subjects taking Cytotec. Importantly, there were no significant differences in the occurrence of these events between the Cytotec group and the placebo group. This information underscores the safety and tolerability of Cytotec, even among elderly patients.
Study No. 1:
- Cytotec 200 mcg q.i.d. (n=74): 4-week therapy - 1 (1.3%), 7-week therapy - 0, 11-week therapy - 0
- Cytotec 100 mcg q.i.d. (n=76): 4-week therapy - 3 (3.7%), 8-week therapy - 1 (1.3%), 12-week therapy - 1 (1.3%)
- Placebo (n=76): 4-week therapy - 11 (14.3%), 8-week therapy - 4 (5.3%), 12-week therapy - 4 (5.2%)
Study No. 2:
- Cytotec 200 mcg q.i.d. (n=60): 4-week therapy - 1 (1.4%), 8-week therapy - 1 (1.5%), 12-week therapy - 0
- Cytotec 100 mcg q.i.d. (n=60): 4-week therapy - 2 (3.0%), 8-week therapy - 2 (3.0%), 12-week therapy - 1 (1.5%)
- Placebo (n=62): 4-week therapy - 6 (9.5%), 8-week therapy - 2 (3.2%), 12-week therapy - 3 (4.8%)
Combined Data (Studies No. 1 & No. 2):
- Cytotec 200 mcg q.i.d. (n=135): 4-week therapy - 2 (1.3%), 8-week therapy - 1 (0.7%), 12-week therapy - 0
- Cytotec 100 mcg q.i.d. (n=140): 4-week therapy - 5 (3.4%), 8-week therapy - 3 (2.1%), 12-week therapy - 2 (1.3%)
- Placebo (n=138): 4-week therapy - 17 (12.2%), 8-week therapy - 6 (4.3%), 12-week therapy - 7 (5.1%)
Cytotec oral tablets pack a punch with either 100 mcg or 200 mcg of misoprostol, a synthetic prostaglandin E1 analog. This active ingredient, misoprostol, is a chemical marvel containing roughly equal amounts of two diastereomers, each with its enantiomers indicated by (±).
In its pharmaceutical form, misoprostol takes the shape of a water-soluble, viscous liquid. But within the Cytotec tablet, it's expertly combined with other key components to create a potent medical solution.
The inactive ingredients within these tablets include hydrogenated castor oil, hypromellose, microcrystalline cellulose, and sodium starch glycolate. These components work in harmony to deliver the medication effectively while ensuring its stability and safety for use. It's this meticulous formulation that makes Cytotec a reliable choice for various medical purposes.
Cytotec Tablets: Identifying and Storing
If you're ever in need of Cytotec tablets, it's essential to know how to recognize and store them properly. These tablets come in two variations: 100-mcg and 200-mcg, each with distinct characteristics.
- Appearance: White and round
- Imprints: You'll find "SEARLE" debossed on one side and "1451" on the other side.
- NDC Number 0025-1451-60: Unit-of-use bottle containing 60 tablets
- NDC Number 0025-1451-20: Unit-of-use bottle containing 120 tablets
- NDC Number 0025-1451-34: Carton containing 100 unit dose tablets
- Appearance: White and hexagonal
- Imprints: "SEARLE" is debossed above, and "1461" is debossed below a line on one side, while the other side features a double stomach imprint.
- NDC Number 0025-1461-60: Unit-of-use bottle containing 60 tablets
- NDC Number 0025-1461-31: Unit-of-use bottle containing 100 tablets
- NDC Number 0025-1461-34: Carton containing 100 unit dose tablets
When it comes to storage, ensure you keep these tablets in a dry area at or below 25°C (77°F). Proper storage guarantees their effectiveness and safety for when you need them most.
How to Take Cytotec
It's crucial to follow your doctor's instructions precisely when taking Cytotec. If you have any doubts or uncertainties, consult your doctor or pharmacist for clarification. Here are the key guidelines for taking Cytotec:
Take with Food: Cytotec should always be taken with food.
Adults Only: This medication is suitable for adults aged 18 years and older.
For Healing Stomach or Duodenal Ulcers:
Normally, you should take two 200 microgram Cytotec tablets twice a day, and this should be done with food. Alternatively, you can opt to take one Cytotec tablet four times a day, spaced at regular intervals, and always with food.
The typical treatment duration for ulcers is 4 weeks, but your doctor may extend it up to 8 weeks if necessary. If your ulcers are not fully healed after this period, further treatment may be recommended.
To Prevent Ulcers When Taking NSAID Medicines:
Your dosage will depend on your specific needs, and your doctor will adjust it accordingly. Generally, you will usually take one 200 microgram tablet, two, three, or four times a day. Your doctor will determine the appropriate dose for you.
Continue taking Cytotec for as long as it is necessary to protect your stomach or gut. You should not stop taking the tablets unless your doctor advises you to do so.
If You Take Too Much Cytotec:
- If you accidentally take too many tablets, contact your doctor or visit the accident and emergency department immediately.
If You Forget to Take Cytotec:
- If you forget to take a dose of your tablets, take them as soon as you remember. However, if it's nearly time for your next scheduled dose, skip the missed tablet(s).
Cytotec's Potential Side Effects
Cytotec, while beneficial for various medical purposes, can sometimes bring about side effects that are important to be aware of. These side effects have been reported in individuals who have used Cytotec:
Diarrhea and Abdominal Pain: In clinical trials, patients receiving Cytotec at doses of 400 or 800 mcg daily frequently experienced diarrhea and abdominal pain. The incidence of diarrhea at 800 mcg ranged from 14-40%, averaging 13% across all studies. Abdominal pain occurred in 12-20% of patients in trials involving NSAIDs and approximately 6% in all studies. Notably, there was no consistent difference from the placebo.
Dose-Related Diarrhea: Diarrhea was often related to the dose and typically occurred early in the treatment (around 13 days). It was usually self-limiting, resolving within about 8 days, but in some cases, it necessitated discontinuation of Cytotec (approximately 2% of patients). Rare instances of severe diarrhea leading to dehydration have been reported. Patients with conditions like inflammatory bowel disease or those at risk of severe dehydration should be monitored closely when prescribed Cytotec. Administering the medication after meals and at bedtime and avoiding its coadministration with magnesium-containing antacids can help minimize the risk of diarrhea.
- Gynecological Disorders: Women who participated in clinical trials while taking Cytotec reported gynecological issues such as spotting (0.7%), cramps (0.6%), hypermenorrhea (0.5%), menstrual disorders (0.3%), and dysmenorrhea (0.1%). Postmenopausal vaginal bleeding may also be associated with Cytotec use, and if it occurs, diagnostic assessment is recommended to rule out any gynecological problems.
Elderly Patients: Studies indicated no significant differences in the safety profile of Cytotec in elderly patients (65 years and older) compared to younger patients.
Additional Adverse Events: Other adverse events reported during clinical trials are categorized as follows:
Incidence Greater Than 1%:
- Nausea (3.1%)
- Flatulence (2.7%)
- Headache (2.2%)
- Dyspepsia (2.1%)
- Vomiting (1.2%)
- Constipation (1.1%)
However, there were no substantial differences in the occurrence of these events between Cytotec and placebo groups.
Causal Relationship Unknown: Some adverse events were infrequently reported, and a clear causal relationship between Cytotec and these events has not been established, but it cannot be entirely ruled out. These events include:
- General body symptoms: aches/pains, asthenia, fatigue, fever, chills, rigors, weight changes.
- Skin issues: rash, dermatitis, alopecia, pallor, breast pain.
- Special senses: abnormal taste, abnormal vision, conjunctivitis, deafness, tinnitus, earache.
- Respiratory problems: upper respiratory tract infection, bronchitis, bronchospasm, dyspnea, pneumonia, epistaxis.
- Cardiovascular issues: chest pain, edema, diaphoresis, hypotension, hypertension, arrhythmia, phlebitis, increased cardiac enzymes, syncope, myocardial infarction (some fatal), thromboembolic events (e.g., pulmonary embolism, arterial thrombosis, and CVA).
- Gastrointestinal problems: GI bleeding, GI inflammation/infection, rectal disorder, abnormal hepatobiliary function, gingivitis, reflux, dysphagia, amylase increase.
- Hypersensitivity reactions: anaphylactic reaction.
- Metabolic abnormalities: glycosuria, gout, increased nitrogen, increased alkaline phosphatase.
- Genitourinary issues: polyuria, dysuria, hematuria, urinary tract infection.
- Nervous system/Psychiatric symptoms: anxiety, change in appetite, depression, drowsiness, dizziness, thirst, impotence, loss of libido, sweating increase, neuropathy, neurosis, confusion.
- Musculoskeletal problems: arthralgia, myalgia, muscle cramps, stiffness, back pain.
- Blood/Coagulation issues: anemia, abnormal differential, thrombocytopenia, purpura, increased ESR (erythrocyte sedimentation rate).
It's important for individuals using Cytotec to be aware of these potential side effects and to consult with their healthcare providers if they experience any adverse reactions.
Warnings and Precautions for Cytotec
BOXED WARNINGS: Please refer to the boxed warnings provided with Cytotec for essential safety information.
Hospital Use Only: Cytotec should only be used in a hospital setting if it is employed for cervical ripening, induction of labor, or the treatment of severe post-partum hemorrhage. These applications are outside of the approved indication.
- Cardiovascular Disease: Exercise caution when administering Cytotec (misoprostol) to patients with pre-existing cardiovascular disease.
Information for Patients:
Women of Childbearing Potential: Women using Cytotec to reduce the risk of NSAID-induced ulcers should be informed that they must not be pregnant when starting Cytotec therapy. They should also be advised to use effective contraception while taking Cytotec.
BOXED WARNINGS: Patients should carefully read the boxed warnings provided with Cytotec for critical safety information.
Proper Use: Cytotec should be taken precisely as directed by a physician. If patients have any questions or encounter issues while taking Cytotec, they should promptly contact their physician.
Not for Others: Patients should not give Cytotec to anyone else. The prescription of Cytotec is specific to the patient's condition and may not be suitable for another individual. Additionally, it could be dangerous to that person if they were to become pregnant.
Patient Information Leaflet: The Cytotec package dispensed by the pharmacist includes a leaflet containing patient information. Patients should read this leaflet before taking Cytotec and whenever they renew their prescription, as it may have been updated.
Keep Out of Reach of Children: It is imperative to store Cytotec out of the reach of children.
Special Note for Women:
- Pregnancy: Cytotec may have adverse effects on pregnancy, potentially causing birth defects, abortion (sometimes incomplete), premature labor, or uterine rupture when given to pregnant women. Pregnant women should not use Cytotec.
Carcinogenesis, Mutagenesis, Impairment of Fertility:
In animal studies, Cytotec did not show evidence of causing tumors or affecting tumor occurrence.
The mutagenic potential of Cytotec was tested in various in vitro assays, all of which yielded negative results.
When administered to breeding male and female rats at high doses, Cytotec resulted in pre-and post-implantation losses and a decrease in live pups born at the highest dose, suggesting a potential adverse effect on fertility in both males and females.
Teratogenic Effects: Please refer to the boxed warnings for information regarding teratogenic effects of Cytotec.
Nonteratogenic Effects: Cytotec may pose risks to pregnancy, including abortion, uterine contractions, uterine bleeding, and expulsion of the products of conception. Abortions caused by Cytotec may be incomplete, and discontinuation of the drug is necessary if a woman becomes pregnant while using it.
Labor and Delivery:
Cytotec can induce or augment uterine contractions. Its use in obstetrics has been associated with adverse effects, including uterine tachysystole, uterine rupture, amniotic fluid embolism, and adverse fetal heart changes. Monitoring of uterine activity and fetal status is essential when using Cytotec in labor.
The risk of uterine rupture increases with advancing gestational age, prior uterine surgery (including Cesarean section), and grand multiparity.
Cytotec should not be used in the third trimester in women with a history of Cesarean section or major uterine surgery, and it should be used cautiously in specific situations.
- Misoprostol, the active component in Cytotec, is excreted in breast milk. While there are no reported adverse effects on breastfed infants, caution is advised when administering Cytotec to nursing women.
- The safety and effectiveness of Cytotec in pediatric patients have not been established.
- Absorption: Misoprostol, the active component of Cytotec, is extensively absorbed after oral administration.
- De-esterification: After absorption, it undergoes rapid de-esterification to its active free acid form, which is responsible for its clinical effects. This free acid form is detectable in the plasma.
- Metabolism: The alpha side chain undergoes beta oxidation, and the beta side chain undergoes omega oxidation, followed by the reduction of the ketone to give prostaglandin F analogs.
- Rapid Absorption: In normal volunteers, Cytotec is rapidly absorbed, with a Tmax (time to reach maximum concentration) of misoprostol acid at approximately 12 ± 3 minutes.
- Half-Life: The terminal half-life of misoprostol acid ranges from 20 to 40 minutes.
- Variability: There is high variability in plasma levels of misoprostol acid between and within studies. However, mean values after single doses show a linear relationship with the dose within the range of 200–400 mcg.
- Accumulation: Multiple dose studies did not show accumulation of misoprostol acid, and plasma steady state was achieved within two days.
- Effect of Food: Maximum plasma concentrations of misoprostol acid are reduced when the dose is taken with food. Concomitant use of antacids also reduces total availability of misoprostol acid.
- Excretion: After oral administration, about 80% of detected radioactivity appears in urine.
- Renal Impairment: Patients with varying degrees of renal impairment may experience approximately twice the half-life (T½), Cmax, and AUC of misoprostol acid compared to normal individuals. However, there is no clear correlation between the degree of impairment and AUC.
- Elderly: In subjects over 64 years of age, the AUC for misoprostol acid is increased.
- Drug Interactions: Misoprostol did not have a significant effect on the kinetics of certain nonsteroidal anti-inflammatory drugs (NSAIDs) like ibuprofen or diclofenac. There was a 20% decrease in aspirin AUC, but this decrease was not considered clinically significant. No significant drug interactions were observed with antipyrine and propranolol when co-administered with misoprostol.
- Serum Protein Binding: The serum protein binding of misoprostol acid is less than 90% and is concentration-independent in the therapeutic range.
Breast Milk Excretion:
- Misoprostol acid, the active form of the drug, is excreted in breast milk.
- The maximum concentration of misoprostol acid in breast milk was achieved within 1 hour after dosing.
- Concentrations in breast milk were 7.6 pg/ml (CV 37%) and 20.9 pg/ml (CV 62%) after single 200 μg and 600 μg misoprostol administrations, respectively.
- Misoprostol acid concentrations in breast milk declined to less than 1 pg/ml at 5 hours post-dose.
Antisecretory and Mucosal Protective Properties:
- Misoprostol exhibits both antisecretory (inhibition of gastric acid secretion) and, in animal studies, mucosal protective properties.
- NSAIDs (nonsteroidal anti-inflammatory drugs) inhibit prostaglandin synthesis, and a deficiency of prostaglandins within the gastric mucosa can lead to reduced bicarbonate and mucus secretion, contributing to mucosal damage caused by these drugs.
- Misoprostol has been shown to increase bicarbonate and mucus production in humans, but this effect has been observed at doses of 200 mcg and above, which are also antisecretory.
- It is challenging to determine whether misoprostol's ability to reduce the risk of gastric ulcers is primarily due to its antisecretory effect, its mucosal protective effect, or a combination of both.
- In vitro studies conducted on canine parietal cells using tritiated misoprostol acid as the ligand have led to the identification and characterization of specific prostaglandin receptors.
- These specific receptors have a high affinity for misoprostol, its acid metabolite, and other E type prostaglandins, but they do not bind well to F or I prostaglandins or unrelated compounds like histamine or cimetidine.
- The affinity of receptor sites for misoprostol correlates with an indirect index of antisecretory activity.
- This specific receptor binding suggests that misoprostol, when taken with food, can effectively target these receptors topically, even though lower serum concentrations are achieved.
Pepsin Concentration and Gastric Acid Secretion:
- Misoprostol produces a moderate decrease in pepsin concentration during basal conditions but not during histamine stimulation.
- It has no significant effect on fasting or postprandial gastrin levels, nor does it affect intrinsic factor output.
Effects on Gastric Acid Secretion:
- Over a range of 50–200 mcg, misoprostol inhibits basal and nocturnal gastric acid secretion and acid secretion in response to various stimuli, including meals, histamine, pentagastrin, and coffee.
- The onset of activity is typically observed around 30 minutes after oral administration, and the effects persist for at least 3 hours.
- The 200-mcg dose has more substantial effects on nocturnal secretion and on histamine and meal-stimulated secretion compared to the 50-mcg dose, which has modest and shorter-lived effects.
- Cytotec has been shown to produce uterine contractions, which can pose a risk to pregnancy (see BOXED WARNINGS).
Other Pharmacologic Effects:
- Misoprostol does not produce clinically significant effects on the serum levels of various hormones, including prolactin, gonadotropins, thyroid-stimulating hormone, growth hormone, thyroxine, cortisol, gastrointestinal hormones (such as somatostatin, gastrin, vasoactive intestinal polypeptide, and motilin), creatinine, or uric acid.
- It does not significantly impact gastric emptying, immunologic competence, platelet aggregation, pulmonary function, or the cardiovascular system at recommended doses.
- In short-term placebo-controlled studies in healthy human volunteers (approximately 1 week in duration), misoprostol was evaluated for its ability to reduce the risk of mucosal injury induced by NSAIDs.
- Misoprostol at doses of 200 mcg q.i.d. when co-administered with tolmetin, naproxen, and ibuprofen showed a reduction in the rate of significant endoscopic injury compared to placebo.
- Doses ranging from 25 to 200 mcg q.i.d. also reduced mucosal injury and bleeding caused by aspirin.
- In 12-week, double-blind trials involving osteoarthritic patients taking NSAIDs, the 200-mcg dose of Cytotec significantly reduced the formation of gastric ulcers. The 100-mcg dose was somewhat less effective, with a significant result in only one of the studies.
- However, Cytotec did not demonstrate effectiveness in reducing the risk ofduodenal ulcers in these trials.
WHO Alert: Falsified Cytotec Poses Serious Health Risks
In a recent WHO Medical Product Alert, two batches of falsified CYTOTEC (misoprostol) 200 microgram tablets have been identified in the WHO Region of Africa. These counterfeit products were reported to WHO in July 2023. The genuine manufacturer of CYTOTEC has confirmed that the products listed in this alert are falsified due to their failure in laboratory analysis and the presence of falsified variable data.
These falsified CYTOTEC products have been detected at both wholesale and patient levels in multiple African countries, including Cameroon, the Democratic Republic of Congo, Ghana, and Nigeria. It's essential to note that Misoprostol is a critical medication listed on the WHO Model List of Essential Medicines. Genuine Cytotec (misoprostol) serves various medical purposes, including the treatment of duodenal and gastric ulcers, induction of labor, prevention of postpartum hemorrhage, treatment of missed and incomplete miscarriages, induction of abortion, and cervical preparation before uterine instrumentation.
The use of falsified Cytotec (misoprostol) poses a significant risk to patient health. Such counterfeit medication can result in ineffective or delayed treatment for the mentioned medical conditions, which, in some cases, can be life-threatening. Therefore, it is crucial to promptly identify and remove any falsified Cytotec (misoprostol) from circulation to protect the well-being of patients.
The products mentioned in this alert are confirmed as falsified because they deliberately and fraudulently misrepresent their identity, composition, or source. Specifically:
Batch B16519: The batch number does not correspond to genuine manufactured CYTOTEC. Laboratory analysis of samples has also revealed that this product lacks any active ingredient and does not comply with specifications.
Batch 14660: The expiry date (7/2023) on this product has been falsified.
In light of this alarming situation, regulatory authorities and the public are strongly advised to exercise caution and vigilance when dealing with Cytotec (misoprostol) products. Any suspicious or counterfeit products should be reported promptly to ensure patient safety and the integrity of healthcare systems.
FAQ; Cytotec (Misoprostol)
1. How Does Cytotec Work for Abortion?
When used for medical abortion, Cytotec plays a crucial role in inducing uterine contractions. It helps terminate an early pregnancy by causing the uterus to expel its contents. This two-step process, involving Mifepristone followed by Misoprostol, is considered a safe and effective method for terminating pregnancies within the first ten weeks.
2. Is Cytotec Safe for Abortion?
When used according to medical guidelines, Cytotec is generally considered safe and effective for medical abortion. However, it should only be administered under the supervision of a qualified healthcare provider to minimize risks and ensure the procedure's success. Self-administration without medical guidance can be dangerous.
3. What Are the Common Side Effects of Cytotec?
Like any medication, Cytotec can have side effects. Common side effects may include abdominal pain, diarrhea, nausea, and mild fever. These side effects are usually temporary and subside on their own. If you experience severe or prolonged side effects, it's essential to seek medical attention promptly.
4. Can Cytotec Be Used for Cervical Ripening?
Yes, Cytotec is also used for cervical ripening in preparation for certain medical procedures, such as induced labor or dilation and curettage (D&C). It helps soften the cervix, making it easier for healthcare providers to perform these procedures safely and effectively.
5. How Should Cytotec Be Taken?
The dosing and administration of Cytotec depend on the specific medical condition it is being used for. It is crucial to follow your healthcare provider's instructions precisely. Generally, Cytotec is taken orally or inserted vaginally, and the dosage varies based on the intended purpose.
6. Is Cytotec Available Over-the-Counter?
No, Cytotec is not available over-the-counter. It is a prescription medication that should only be obtained and used under the supervision of a licensed healthcare provider.
7. Can Cytotec Cause Allergic Reactions?
While allergic reactions to Cytotec are rare, they are possible. If you develop symptoms such as rash, itching, swelling, severe dizziness, or difficulty breathing after taking Cytotec, seek immediate medical attention, as these could be signs of an allergic reaction.
8. Are There Any Drug Interactions with Cytotec?
Cytotec may interact with other medications, potentially affecting its effectiveness or safety. It's essential to inform your healthcare provider about all the medications you are currently taking to ensure there are no adverse interactions.
9. Can Cytotec Be Used for Off-Label Purposes?
Some healthcare providers may prescribe Cytotec for off-label uses, which are uses not specifically approved by regulatory agencies. These off-label uses may include treating conditions such as postpartum hemorrhage or cervical priming for IUD insertion. Always follow your healthcare provider's guidance regarding off-label use.
Medical Facts 2023
Safety and Supervision: The safe and effective use of Cytotec, especially in abortion procedures, requires strict medical supervision. Self-administration without professional guidance can be risky and is not recommended.
Allergic Reactions: While rare, allergic reactions to Cytotec can occur. Symptoms such as rash, itching, swelling, severe dizziness, or difficulty breathing should be reported to a healthcare provider immediately.
Prescription Medication: Cytotec is not available over-the-counter and is strictly a prescription medication. It should only be obtained and used under the supervision of a licensed healthcare provider.
Drug Interactions: Cytotec may interact with other medications, potentially affecting its safety or effectiveness. Patients should inform their healthcare provider of all medications they are taking.
Off-Label Uses: In some cases, healthcare providers may prescribe Cytotec for off-label uses, such as cervical ripening for certain medical procedures. Always follow your healthcare provider's recommendations in these situations.
Ongoing Research: Research into the safety and efficacy of Cytotec continues, and healthcare guidelines may evolve over time based on new findings and clinical studies.