Name of the Abortifacients Drugs
- Corboprost
- Dinoprostone
- Mifepristone
Therapeutic Action
To stimulate uterine activity, dislodging any implanted trophoblasts and preventing implantation of any fertilized egg
| CARBOPROST |
| Availability : carboprost tromethamine injectable solution : 250mcg/ml in 1ml ampoule and 10ml vial. |
| Administration and Handling : should be administered as a deep intramuscular injection. Vials are for single use only and any residue should be discarded. Storage requirements: Refrigerate at 2C to 8C (36F to 46F) |
| Abortion: Initial dose: 250 mcg (1 mL) once by deep IM injection, with a tuberculin syringe. Subsequent doses of 250 mcg (1 mL) may be administered at 1.5 to 3.5 hour intervals depending on uterine response. An optional test dose of 100 mcg (0.4 mL) may be administered initially. The dose may be increased to 500 mcg (2 mL) if uterine contractility is judged to be inadequate after several doses of 250 mcg (1 mL). Maximum total dose: 12 mg Duration of therapy: No more than 2 continuous days. |
| Postpartum Bleeding: Initial dose: 250 mcg (1 mL) once by deep IM injection. Additional doses can be administered at intervals of 15 to 90 minutes, if necessary. Maximum total dose: 2 mg (8 doses) Comments: The need for additional injections and the administration interval should be determined by the attending physician as dictated by the course of clinical events. |
Mechanism of Action:
Inhibits or stimulates smooth muscle contraction, which results in expulsion of the products of conception and is used to induce abortion between 13-20 weeks of pregnancy; inhibits release of norepinephrine or modulates its effects at neuroeffector sites
Indications:
- Aborting pregnancy between the 13 th and 20 th weeks of gestation (calculated from the first day of the last normal menstrual period)
- Failure of expulsion of the fetus during the course of treatment by another method
- Premature rupture of membranes in intrauterine methods with loss of drug and insufficient or absent uterine activity
- Requirement of a repeat intrauterine instillation of drug for expulsion of the fetus
- Inadvertent or spontaneous rupture of membranes in the presence of a previable fetus and absence of adequate activity for expulsion
- Refractory postpartum hemorrhage due to uterine atony that has not responded to conventional methods of management
Contraindications & Cautions:
- Known hypersensitivity to carboprost.
- Acute pelvic inflammatory disease.
- Active cardiac, pulmonary, renal, or hepatic disease.
Caution
- In patients with anemia, jaundice, renal impairment, hepatic impairment diabetes or epilepsy
- History of glaucoma or raised IOP
- Asthma, hypertension/hypotension, cardiovascular disease
Metabolism and Half- Life :
- Peak plasma time: 20-30 min
- Concentration: 1-1.6 ng/mL
- Half-life: 3 hr
- Protein bound: None
- Excretion: Urine
Drug Interactions:
Concomitant use with other oxytocic agents is not recommended.
Side- Effects:
- Diarrhea (most common, may be sudden in onset)
- Flushing or hot flashes
- Fever
- Chills
- Nausea/vomiting
- Urinary tract infection
- Uterine bleeding (excessive)
- Uterine rupture
- Uterine sacculation
- Local: injection site pain
- Flushing
- Asthma
- Wheezing
- Coughing
- Chest pain
Nursing Considerations
- Only medically trained personnel should administer the product in a hospital setting that can provide immediate care and acute surgical facilities
- Potent oxytocic agent; use strict adherence to recommended dosing
- To decrease GI side effects pretreatment or concomitant use with antiemetic and antidiarrheal agents recommended
- This drug should not be given intravenously.
- Carboprost is not indicated if the fetus has reached the stage of viability.
- Risk of cervical trauma; examine each patient for cervical injuries after abortion is complete. Caution in patients with a compromised (scarred) uterus.
- Carefully monitor the vital signs and contractions frequently as this drug may cause changes in temperature and BP.
- Should not be used for the induction of labour.
- Parenteral drug products should be inspected visually for particulate matter and discolouration prior to administration.
- Watch for Heavy bleeding. Cervix should be checked after the procedure.
Patient/ Family education
- Importance of women informing clinicians if they plan to breast-feed.
- Importance of informing clinicians of existing or contemplated concomitant therapy, including prescription and OTC drugs, as well as any concomitant illnesses.
- Importance of informing patients of other important precautionary information.
- Do not drive, use any tools or operate machinery soon after receiving Hemabate as it may affect your ability to do so safely. Hemabate may make you lose consciousness, feel dizzy or drowsy.
- Teach the client about the possible side effects and when to seek medical help.
| DINOPROSTONE |
| Availability: Endocervical gel: 0.5 mg in 3-g gel vehicle in prefilled syringe with catheter Vaginal insert: 10 mg Vaginal suppositories: 20 mg |
| Administration and Handling: Keep patient supine for 15 to 30 minutes after gel administration and for 10 minutes after administering suppository to prevent drug expulsion. Store suppositories in freezer; bring to room temperature before using. The cervical gel has a more rapid release than the vaginal insert but might be less convenient, as the procedure requires more vaginal examinations. |
| Cervical ripening: Adults: 0.5 mg endocervical gel vaginally; if response is poor, may repeat in 6 hours (not to exceed 1.5 mg in 24 hours). Or one 10-mg vaginal insert. |
| To induce abortion : Adults: One 20-mg vaginal suppository; repeat q 3 to 5 hours (not to exceed total dosage of 240 mg or duration of 48 hours). |
| Nonmetastatic gestational trophoblastic disease (benign hydatidiform mole) : Adults: Insert one 20-mg suppository high into vagina; may repeat at 3- to 5-hour intervals for up to 2 days if necessary. |
Mechanism of Action:
Initiates strong contractions of uterine smooth muscle by stimulating myometrium and promoting cervical softening, effacement, and dilation.
Indications:
- Cervical ripening
- To induce abortion
- Nonmetastatic gestational trophoblastic disease (benign hydatidiform mole)
Contraindications and Cautions:
- Hypersensitivity to prostaglandins or additives in gel or suppository
- When vaginal delivery isn’t indicated, such as with vasa previa or active genital herpes infection (Prepidil)
- Acute pelvic inflammatory disease
- Ruptured membranes, placenta previa, marked cephalopelvic disproportion, or unexplained vaginal bleeding during pregnancy
- When oxytocics are contraindicated or when prolonged contraction of uterus may be detrimental to fetal safety or uterine integrity, such as with previous cesarean section or major uterine surgery
- Concurrent use of I.V. oxytocics (Cervidil)
- Clinical suspicion or definite evidence of fetal distress when delivery isn’t imminent (Cervidil, Prepidil)
- History of difficult labor or traumatic delivery, hyperactive or hypertonic uterine patterns (Prepidil)
- Obstetric emergencies in which benefit-to-risk ratio for either fetus or mother favors surgical intervention (Prepidil)
- Active cardiac, pulmonary, renal, or hepatic disease (Prostin E2 Vaginal Suppository)
- Multipara with six or more previous term pregnancies (Cervidil)
- Grand multipara with six or more previous term pregnancies with nonvertex presentation (Prepidil)
Use cautiously in:
- History of pulmonary, cardiac, renal, or hepatic disease
- Asthma
- Jaundice
- Anemia
- Cervicitis
- infected endocervical lesions
- acute vaginitis
- Compromised (scarred) uterus
- hypertension
- Hypotension
- adrenal disorders
- Diabetes mellitus
- Epilepsy
- glaucoma
- women age 30 or older, those with complications during pregnancy, and those with gestational age of more than 40 weeks are at increased risk of post-partum disseminated intravascular coagulation
- concurrent use of other oxytocics (not recommended).
Metabolism and Half- Life:
- Peak plasma time: 0.5-0.75 hr
- Onset: In most first and second trimester pregnancies, slight uterine contractions begin within 10 min
- Duration: Contractions continue for 2-3 hr following vaginal insertion of a dinoprostone suppository
- Metabolism: Rapidly in the maternal lungs, kidneys, spleen, and other tissues, primarily by oxidation of side chains to at least 9 inactive metabolites; Half-life: 2.5-5 min
- Excretion: Urine (principally); feces (small amount)
Drug Interactions:
Other oxytocics: increased oxytocic effects
Side- Effects:
- CNS: headache, drowsiness, syncope
- CV: hypotension, hypertension
- GI: nausea, vomiting, diarrhea
- GU: urinary tract infection, vaginal or uterine pain, uterine contractile abnormalities, warm vaginal sensation, uterine hypertonicity, uterine rupture
- Musculoskeletal: back pain
- Respiratory: cough, dyspnea, wheezing
- Other: allergic reactions including chills, fever, and anaphylaxis
Nursing Considerations
- Administer in hospital setting with obstetric care facility
- Use caution in patients with epilepsy, glaucoma, hepatic/renal impairment, pulmonary disease
- Monitor uterine contractions and observe for excessive vaginal bleeding and cramping. Record sanitary pad count.
- Monitor vital signs and assess for drug-induced fever. Report significant blood pressure and pulse changes.
- Cephalopelvic relationships should be carefully evaluated before the use
- Assess for wheezing, chest pain, and dyspnoea.
- Evaluate for GI upset. To minimize, give antiemetic before dinoprostone therapy.
- Wait 30 min following removal of insert, or 6-12 hr following gel application, before administering other oxytocic drugs
- Do not administer gel above level of internal os
- Remove insert before amniotomy
- Patients should be monitored for adverse effects, especially pyrexia, and the drug should be stopped if any severe adverse reactions occur.
- Abortion via prostaglandin E2 suppository may be incomplete, which may require further measures such as dilation and curettage.
- Uterine activity, fetal status, and progression of cervical dilation all require monitoring. In particular, the healthcare team should look for any signs of uterine hyperstimulation, sustained uterine contractions, and fetal distress. If these or any other adverse effects present, the insert should be removed and drug administration stopped.
Patient/ Family Teaching:
- Advise patient to stay in supine position, as prescribed, after administration.
- Instruct patient to report fever, bleeding, or abdominal cramps.
- Tell patient to avoid douches, tampons, tub baths, and sexual intercourse for at least 2 weeks after receiving drug.
- Inform about the possible side effects
| MIFEPRISTONE |
| Availability: Tablets: 200 mg, 300 mg |
| Administration and Handling: Oral Administration (Mifeprex) 200 mg PO once, followed 24-48 hr later by misoprostol buccal administration. Follow up with healthcare provider 7-14 days after taking Mifeprex Buccal administration (misoprostol) •Because most women will expel the pregnancy within 2-24 hr of taking misoprostol, discuss with the patient an appropriate location for her to be when she takes the misoprostol, taking into account that expulsion could begin within 2 hr of administration •Administer misoprostol 800 mcg buccally within 24-48 hr after taking Mifeprex •The effectiveness of the regimen may be lower if misoprostol is administered <24 hr or >48 hr after mifepristone administration •Tell the patient to place two 200 mcg misoprostol tablets in each cheek pouch (the area between the cheek and gums) for 30 minutes and then swallow any remnants with water or another liquid •During the period immediately following the administration of misoprostol, the patient may need medication for cramps or GI symptoms |
| Oral Administration (Korlym): always take with a meal. Must be taken as a single daily dose. Swallow tablet whole, do not split, crush, or chew; Dose reduction or discontinuation may be needed in some clinical situations; if dosage is interrupted, reinitiate at the lowest dose (ie, 300 mg/day) |
| Before giving dose for termination of pregnancy, make sure patient doesn’t have an IUD in place. Correct hypokalemia before starting Korlym; Give for termination of pregnancy only in health care facility under supervision of health care provider qualified to assess pregnancy stage and rule out ectopic pregnancy. Administer with fluids, but not with grapefruit juice. When giving for termination of pregnancy, confirm pregnancy termination 14 days after initial dose. |
| Termination of intrauterine pregnancy through day 49 of pregnancy: Adults: On day 1, mifepristone 600 mg P.O. as a single dose. On day 3, misoprostol 400 mcg P.O. (unless abortion has been confirmed). |
| Hyperglycemia secondary to hypercortisolism in adults with endogenous Cushing’s syndrome who have type 2 diabetes or glucose intolerance and have failed surgery or aren’t candidates for surgery Adults: Initially, 300 mg P.O. daily; increase based on clinical response and tolerability in 300-mg increments to a maximum of 1,200 mg daily. Don’t exceed 20 mg/kg/day. |
| Pregnancy Termination Mifeprex: Indicated for the medical termination of intrauterine pregnancy through 70 days gestation in combination with misoprostol Day 1: 200 mg of mifepristone PO as a single dose Days 2-3: 800 mcg of misoprostol buccally once as a single dose; must be administered a minimum of 24-hr and a maximum of 48-hr following mifeprostone dose on day 1 (see Administration) Follow up with healthcare provider 7-14 days after taking Mifeprex Days 7-14 •Must return for follow-up visit to confirm complete termination has occurred by medical history, clinical examination, hCG testing, or ultrasonographic scan •If complete expulsion has not occurred, but the pregnancy is not ongoing, women may be treated with another dose of misoprostol 800 mcg buccally with follow-up in ~7 days •Lack of bleeding following treatment usually indicates failure; however, prolonged or heavy bleeding is not proof of a complete abortion •Surgical evacuation is recommended to manage ongoing pregnancies after medical abortion |
| Cushing Syndrome: Korlym: Indicated to control hyperglycemia secondary to hypercortisolism in adults with endogenous Cushing syndrome who have type 2 diabetes mellitus or glucose intolerance and have failed surgery or are not candidates for surgery 300 mg PO qDay initially; may dose to a maximum of 1200 mg/day, but should not exceed 20 mg/kg/day Increase in dose should not occur more frequently than every 2-4 weeks and should be based on assessment of glucose control, antidiabetic medication requirements, insulin levels and psychiatric symptoms. |
Mechanism of Action:
Antagonizes progesterone receptor sites, inhibiting activity of endogenous and exogenous progesterone and stimulating uterine contractions, which causes fetus to separate from placental wall
Indications:
- Termination of intrauterine pregnancy through day 49 of pregnancy
- Hyperglycemia secondary to hypercortisolism in adults with endogenous Cushing’s syndrome who have type 2 diabetes or glucose intolerance and have failed surgery or aren’t candidates for surgery
- Cushing Syndrome
Contraindications & Cautions :
- Hypersensitivity to drug, misoprostol, or other prostaglandins
- Confirmed or suspected ectopic pregnancy or adnexal mass
- Chronic adrenal failure
- Bleeding disorders
- Concurrent anticoagulant therapy or long-term corticosteroid therapy
- Presence of intrauterine device (IUD)
- Inherited porphyrias
- Concomitant treatment with systemic corticosteroids for serious medical conditions or illnesses (Korlym)
- Concurrent use of simvastatin or lovastatin and CYP3A substrates with narrow therapeutic range (Korlym)
- History of unexplained vaginal bleeding or endometrial hyperplasia with atypia or endometrial carcinoma (Korlym)
- Pregnancy (Korlym)
Use cautiously in:
- Cardiovascular, respiratory, renal, or hepatic disorders; hypertension; type 1 diabetes mellitus; anemia; jaundice; seizure disorder; cervicitis; infected endocervical lesions; acute vaginitis; uterine scarring
- Hypokalemia, underlying heart conditions including heart failure and coronary vascular disease (Korlym)
- Hemorrhagic disorders or concurrent use of anticoagulants (korlym)
- Concurrent use of QT interval-prolonging drugs, patients with potassium channel variants resulting in long QT interval (avoid korlym use)
- Concurrent use of drugs metabolized by CYP2B6 and moderate CYP3A inhibitors (korlym)
- Concurrent use of CYP3A inducers (such as rifampin, rifabutin, rifapentin, phenobarbital, phenytoin, carbamazepine, and st. John’s wort) or hormonal contraceptives (avoid use)
- Concurrent use of strong CYP3A inhibitors (use korlym with extreme caution and only when necessary; limit dosage to 300 mg)
- Concurrent use of drugs metabolized by CYP2C8/2C9 (use lowest dose of CYP2C8/2C9 substrates when used with korlym)
- Breastfeeding patients (korlym)
- Children (korlym; safety and efficacy not established).
Metabolism and Half-life:
Absorption: Peak Plasma Time: 1-2 hr (single dose); 1-4 hr (multiple doses); Peak Plasma Concentration: 2-8 hr
Distribution: Protein Bound: >99% to alpha-1-acid glycoprotein; 96-99% (active metabolites)
Distributed to other tissues including CNS
Metabolism: Extensively metabolized by CYP3A4
Metabolized to 3 active metabolites, of which 2 are the product of demethylation, while a third active metabolite results from hydroxylation. In addition to being a CYP3A4 substrate, it also inhibits and induces CYP3A4
Elimination: Half-life: 20 hr (single dose); 85 hr (parent drug following multiple doses); Excretion: 90% feces.
Drug Interactions:
- CYP2C8/2C9 substrates: increased plasma concentrations of these drugs
- CYP3A inducers (such as carbamazepine, phenobarbital, phenytoin, rifabutin, rifampin, rifapentin): decreased mifepristone concentrations
- CYP3A substrates with narrow therapeutic range (such as cyclosporine, dihydroergotamine, ergotamine, fentanyl, pimozide, quinidine, sirolimus, tacrolimus): increased exposure of these drugs and effects
- Drugs metabolized by CYP2B6 (bupropion, efavirenz): significantly increased exposure of these drugs
- Drugs metabolized by CYP3A (lovastatin, simvastatin): increased risk of myopathy and rhabdomyolysis
- Glucocorticoids: antagonized glucocorticoid effect
- Oral contraceptives: decreased oral contraceptive effectiveness
- Hematocrit, hemoglobin: decreased values
- Potassium: decreased level
- Red blood cells: decreased count
- Grapefruit juice: increased mifepristone blood level and effects
Side- Effects:
- CNS: dizziness, fainting, headache, weakness, fatigue, insomnia, asthenia, anxiety, syncope, rigors
- CV: hypertension, QT-interval prolongation (Korlym)
- EENT: sinusitis
- GI: nausea, vomiting, diarrhea, abdominal cramping, dyspepsia
- GU: vaginitis, leukorrhea, uterine cramping, pelvic pain; endometrial hypertrophy, cystic dilatation of endometrial glands, vaginal bleeding (Korlym); uterine hemorrhage
- Hematologic: anemia
- Metabolic: hypokalemia, adrenal insufficiency (Korlym)
- Musculoskeletal: leg pain, back pain, arthralgia
- Skin: rash (Korlym)
- Other: viral infections; fever, decreased appetite, peripheral edema, opportunistic infections (Korlym)
Nursing Considerations
- Assess vital signs, breath sounds, and bowel sounds.
- Monitor uterine contractions and type and amount of vaginal bleeding.
- Evaluate CBC.
- Monitor serum potassium level 1 to 2 weeks after starting or increasing Korlym dosage and periodically thereafter.
- Closely monitor patient taking Korlym for signs and symptoms of adrenal insufficiency, including weakness, nausea, increased fatigue, hypotension, and hypoglycemia. If adrenal insufficiency is suspected, discontinue drug immediately and administer glucocorticoids without delay. May resume Korlym at a lower dosage after resolution of adrenal insufficiency.
- Be aware that patients with endogenous Cushing’s syndrome are at risk for opportunistic infections such as Pneumocystis jiroveci pneumonia while taking Korlym. Monitor patient for respiratory distress shortly after Korlym initiation. Initiate appropriate diagnostic tests and treat P. jiroveci as indicated.
Patient /Family teaching
When used for termination of pregnancy:
- After administration, tell patient she will need to return in 48 hours for a prostaglandin drug or to verify pregnancy termination.
- Tell patient she will have contractions for 3 or more hours after receiving drug and that vaginal bleeding may last 9 to 16 days.
- Instruct patient to contact prescriber if she has persistent or extremely heavy vaginal bleeding, extreme fatigue, or orthostatic hypotension.
- Caution patient that vaginal bleeding does not prove that complete abortion has occurred. Tell her she will need follow-up appointment 2 weeks later to verify pregnancy termination.
- Inform patient that she is at risk for pregnancy right after abortion is complete. Encourage appropriate contraceptive decision.
When used for hyperglycemia secondary to hypercortisolism in patients with endogenous Cushing’s syndrome:
- Instruct patient to recognize and report signs and symptoms of hypokalemia, respiratory infections, and adrenal insufficiency.
- Advise patient not to take drug with grapefruit juice and not to use herbal products without consulting prescriber.
REFERENCES
- Mc Graw-Hill Nurse’s Drug Handbook- 7th edition
- Jones & Bartlett Learning Nurse’s Drug Handbook – 10th Edition –2011
- Saunders Nursing Drug Handbook 2021 (Robert J. Kizior, Keith Hodgson)
- https://www.rnpedia.com/nursing-notes/pharmacology-drug-study-notes/drugs-for-female-reproductive-system/
- https://reference.medscape.com
- https://www.evanspharmacy.com
- https://www.lupinhealthcare.co.uk
- https://en.wikipedia.org
- https://medicalguidelines.msf.org
- https://go.drugbank.com
- https://www.mims.com
- https://www.ferring.ca
- https://www.accessdata.fda.gov
- https://pubchem.ncbi.nlm.nih.gov
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