Ethinylestradiol + Drospirenone


Thông tin thuốc gốc
Chỉ định và Liều dùng
Oral
Contraception
Adult: Available preparations:
Ethinylestradiol 0.02 mg and drospirenone 3 mg tab
Ethinylestradiol 0.03 mg and drospirenone 3 mg tab

1 tab once daily, exactly as directed from the blister pack. Doses must be taken continuously at the same time each day. Refer to the detailed product guideline on how to manage missed doses and for other dosing instructions.

Oral
Acne vulgaris
Adult: Available preparation:
Ethinylestradiol 0.02 mg and drospirenone 3 mg tab

For women with moderate acne who desires oral contraceptive for birth control: 1 tab once daily, exactly as directed from the blister pack. Doses must be taken continuously at the same time each day. Refer to the detailed product guideline on how to manage missed doses and for other dosing instructions.
Child: ≥14 years For those who have achieved menarche: Same as adult dose.

Oral
Premenstrual dysphoric disorder
Adult: Available preparation:
Ethinylestradiol 0.02 mg and drospirenone 3 mg tab

For women who choose oral contraceptive as method of contraception: 1 tab once daily, exactly as directed from the blister pack. Doses must be taken continuously at the same time each day. Refer to the detailed product guideline on how to manage missed doses and for other dosing instructions.
Renal Impairment
Contraindicated.
Hepatic Impairment
Contraindicated.
Cách dùng
May be taken with or without food. Take at the same time each day, preferably after evening meal or at bedtime.
Chống chỉ định
Adrenal insufficiency, current, suspected or history of breast cancer or other oestrogen- or progestin-sensitive cancer; presence of severe or multiple risk factors for venous or arterial thromboembolism (VTE/ATE) (e.g. DVT, pulmonary embolism, major surgery with prolonged immobilisation, MI, angina pectoris, cerebrovascular disease such as stroke or TIA; headaches with focal neurological symptoms, migraine headaches with or without aura if >35 years, diabetes mellitus with vascular symptoms, severe or uncontrolled hypertension, severe dyslipoproteinaemia, coronary artery disease, inherited or acquired hypercoagulopathies, thrombogenic valvular or heart rhythm diseases such as subacute bacterial endocarditis with valvular disease or atrial fibrillation; women >35 years who smoke, obesity [BMI >30 kg/m2]; known hereditary or acquired predisposition to VTE/ATE such as activated protein C [APC]-resistance, Factor V Leiden mutation, antithrombin-III-deficiency, protein C and S deficiency, hyperhomocysteinaemia, anti-phospholipid antibodies [e.g. anticardiolipin antibodies, lupus anticoagulant]; SLE with unknown or positive antiphospholipid antibodies); presence or history of hepatic tumours (benign or malignant), undiagnosed abnormal uterine/vaginal bleeding, acute viral hepatitis. Renal and hepatic impairment. Pregnancy. Concomitant use with hepatitis C drug combinations containing ombitasvir, paritaprevir/ritonavir with or without dasabuvir.
Thận trọng
Women with risk factors for CV disease (e.g. low HDL, high LDL or triglycerides); depression, prediabetes or diabetes mellitus, hypertriglyceridaemia, history of chloasma gravidarum, SLE, chronic inflammatory bowel disease, hereditary angioedema, history of pregnancy-related cholestasis, who are undergoing thyroid replacement therapy; who undergone specific bariatric procedures (e.g. Roux-en-Y, biliopancreatic diversion). Smokers. Not indicated for use prior to menarche, or in postmenopausal women. Not recommended for women with complicated organ transplants (e.g. graft failure, rejection, cardiac allograft vasculopathy). Lactation.
Phản ứng phụ
Significant: Increased risk of cervical and breast cancer, cholestasis, pancreatitis, gallbladder disease; worsening of depression, Crohn’s disease, and ulcerative colitis; recurrent, persistent or severe headache/migraine; induced or exacerbated angioedema, chloasma, hyperkalaemia, jaundice, unscheduled bleeding (breakthrough or intracyclic), spotting, amenorrhoea, oligomenorrhoea, retinal vein thrombosis, impaired glucose tolerance, adverse lipid level changes (including serum triglycerides), increased thyroid-binding globulin levels, disturbance of LFT. Rarely, increased risk of hepatocellular carcinoma (prolonged use), increased blood pressure.
Cardiac disorders: Rarely, tachycardia.
Eye disorders: Rarely, dry eye, conjunctivitis.
Gastrointestinal disorders: Nausea, abdominal pain, vomiting, diarrhoea, dyspepsia, flatulence, gastritis.
General disorders and admin site conditions: Asthenia, oedema.
Hepatobiliary disorders: Rarely, biliary pain, cholecystitis.
Immune system disorders: Hypersensitivity.
Investigations: Weight increased.
Metabolism and nutrition disorders: Rarely, increased appetite, hyponatraemia.
Musculoskeletal and connective tissue disorders: Back pain, muscle cramps.
Nervous system disorders: Dizziness, paraesthesia.
Psychiatric disorders: Emotional lability, nervousness, somnolence.
Reproductive system and breast disorders: Breast tenderness/pain, metrorrhagia, pelvic pain, breast enlargement, dysmenorrhoea, vaginal discharge, vulvovaginal candidiasis, decreased libido.
Skin and subcutaneous tissue disorders: Acne, rash, pruritus, increased sweating.
Vascular disorders: Hot flushes.
Potentially Fatal: Increased risk of VTE, ATE (e.g. DVT, pulmonary embolism, MI). Rarely, hepatic adenomas or tumours (benign/malignant).
Monitoring Parameters
Evaluate pregnancy (prior to treatment) and smoking status. Perform adequate diagnostic measures to rule out malignancy in case of undiagnosed vaginal bleeding. Monitor blood pressure prior to therapy and yearly; weight/BMI at baseline; vision changes, signs and symptoms of thromboembolic disorders, depression, and bleeding irregularities.
Quá liều
Symptoms: Nausea, vomiting, and withdrawal bleeding. Management: Symptomatic treatment. Monitor serum K and Na levels, and for signs of metabolic acidosis.
Tương tác
May increase risk of breakthrough bleeding and diminished efficacy with CYP3A4 inducers (e.g. rifampicin, barbiturates, bosentan, carbamazepine, phenytoin, primidone, efavirenz, felbamate, griseofulvin, oxcarbazepine, topiramate). May increase the plasma concentrations of ciclosporin. May significantly decrease the plasma levels of lamotrigine. Plasma concentrations may be increased by moderate or strong CYP3A4 inhibitors (e.g. ketoconazole, itraconazole, verapamil, clarithromycin, erythromycin, diltiazem). Increased serum K concentration with ACE inhibitors, angiotensin-II receptor antagonists, K-sparing diuretics, K supplements, heparin, aldosterone antagonists, NSAIDS.
Ethinylestradiol: May inhibit clearance and increase plasma concentrations of CYP1A2 substrates (e.g. theophylline, tizanidine). May elevate plasma levels with ascorbic acid.
Potentially Fatal: Increased risk of ALT elevations with drugs containing ombitasvir, paritaprevir/ritonavir, with or without dasabuvir.
Food Interaction
May increase the risk of breakthrough bleeding and diminished efficacy when given with St. John’s wort. Plasma levels may be increased when given with grapefruit juice.
Lab Interference
May interfere with the results of certain tests for lipids, glucose tolerance, coagulation factors, plasma levels of carrier proteins (e.g. corticosteroid-binding globulin, lipid/lipoprotein fractions), parameters of carbohydrate metabolism and fibrinolysis; liver, renal, thyroid, and adrenal function.
Drospirenone may increase plasma renin activity and plasma aldosterone.
Tác dụng
Description: Ethinylestradiol and drospirenone suppress ovulation by negative feedback mechanism on the hypothalamus that changes the normal gonadotropin secretion pattern of FSH and LH by the anterior pituitary gland, thereby blocking the follicular FSH phase and midcycle surge of gonadotropins. They also alter the tubal transport of the ova through the fallopian tubes and the genital tract. The changes in cervical mucus and in the endometrium lead to inhibition of sperm penetration and unfavourable environment for nidation, respectively.
Ethinylestradiol is a synthetic oestrogen with similar effects to estradiol.
Drospirenone is a structural analogue of spironolactone that has anti-mineralocorticoid and antiandrogenic effects, resembling the natural hormone progesterone.
Pharmacokinetics:
Absorption: Ethinylestradiol: Rapidly and completely absorbed from the gastrointestinal tract. Bioavailability: Approx 40%. Time to peak plasma concentration: 1-2 hours.
Drospirenone: Rapidly and almost completely absorbed from the gastrointestinal tract. Bioavailability: Approx 76-85%. Time to peak plasma concentration: 1-2 hours.
Distribution: Ethinylestradiol: Enters breast milk (small amounts). Volume of distribution: Approx 4-5 L/kg. Plasma protein binding: Approx 98%, mainly to albumin.
Drospirenone: Enters breast milk. Volume of distribution: Approx 4 L/kg. Plasma protein binding: Approx 97% (except to sex hormone and corticosteroid-binding globulin).
Metabolism: Ethinylestradiol: Undergoes significant gut and hepatic first-pass metabolism; metabolised in the liver primarily via aromatic hydroxylation by CYP3A4 isoenzyme to form various hydroxylated and methylated metabolites.
Drospirenone: Extensively metabolised in the liver via opening of lactone ring into the acid form of drospirenone, and via reduction and sulfation into 4,5-dihydro-drospirenone-3-sulfate. Subject to oxidation by CYP3A4 isoenzyme.
Excretion: Ethinylestradiol: Via urine and faeces. Terminal elimination half-life: Approx 24 hours.
Drospirenone: Via urine and faeces. Terminal elimination half-life: Approx 30-40 hours.
Đặc tính

Chemical Structure Image
Ethinylestradiol

Source: National Center for Biotechnology Information. PubChem Database. Ethinyl estradiol, CID=5991, https://pubchem.ncbi.nlm.nih.gov/compound/Ethinyl-estradiol (accessed on Jan. 22, 2020)


Chemical Structure Image
Drospirenone

Source: National Center for Biotechnology Information. PubChem Database. Drospirenone, CID=68873, https://pubchem.ncbi.nlm.nih.gov/compound/Drospirenone (accessed on Jan. 22, 2020)

Bảo quản
Store at 25°C.
Phân loại ATC
G03AA12 - drospirenone and ethinylestradiol ; Belongs to the class of progestogens and estrogens in fixed combinations. Used as systemic contraceptives.
References
Anon. Ethinyl Estradiol and Drospirenone. Lexicomp Online. Hudson, Ohio. Wolters Kluwer Clinical Drug Information, Inc. https://online.lexi.com. Accessed 16/01/2020.

Buckingham R (ed). Drospirenone. Martindale: The Complete Drug Reference [online]. London. Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 16/01/2020.

Buckingham R (ed). Ethinylestradiol. Martindale: The Complete Drug Reference [online]. London. Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 16/01/2020.

Gianvi (Teva Pharmaceuticals USA Inc). DailyMed. Source: U.S. National Library of Medicine. https://dailymed.nlm.nih.gov/dailymed/. Accessed 16/01/2020.

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