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    Summary for UKPID




    PROGESTOGENS




    Helen Seymour, BPharm (Hons)

    National Poisons Information Service (Newcastle Centre)
    Regional Drug & Therapeutics Centre
    Wolfson Building
    Claremont Place
    Newcastle upon Tyne
    NE1 4LP
    UK


    This monograph has been produced by staff of a National Poisons
    Information Service Centre in the United Kingdom.  The work was
    commissioned and funded by the UK Departments of Health, and was
    designed as a source of detailed information for use by poisons
    information centres.

    Peer review group: Directors of the UK National Poisons Information
    Service.


    SUMMARY

    Type of product

         Used for a number of purposes, including treatment of amenorrhea,
         abnormal uterine bleeding, contraception, malignant disease and
         menopausal symptoms.

    Ingredients

         A progestogen.

    Toxicity

         Very low.

    Features

         May cause nausea and vomiting.
         Rarely, withdrawal bleeding may occur in pre-pubertal girls.

    Treatment

         None required.

    SUBSTANCE

         Progestogen

    ORIGIN OF SUBSTANCE

         Synthetic

    NAME

    Brand Name/Generic Name
         Cyclogest/ Progesterone
         Depo-Provera/Medroxyprogesterone
         Depostat/ Gestronol hexanoate
         Duphaston/ Dydrogesterone
         Duphaston HRT/Dydrogesterone
         Farlutal/ Medroxyprogesterone
         Femulen/ Ethynodiol diacetate
         Gestone/ Progesterone
         Megace/ Megesterol Acetate
         Menzol/ Norethisterone
         Micronor HRT/ Norethisterone
         Micronor/ Norethisterone
         Microval/ Levonorgestrel
         Mirena/Levonorgestrel
         Neogest/ Norgestrel
         Norgeston/ Levonorgestrel

         Noriday/ Norethisterone
         Noristat/ Norethisterone
         Norplant/ Levonorgestrel
         Primolut N/ Norethisterone
         Proluten Depot/ Hydroxyprogesterone Hexanoate
         Provera/ Medroxyprogesterone Acetate
         Utovlan/ Norethisterone

    CHEMICAL GROUP

         Progestogens
         BNF 6.4.1.2
         Progestogen-Only contraceptives
         BNF 7.3.2
         Progestogens
         BNF 8.3.2

    SUBSTANCE IDENTITY

    REFERENCE NUMBER

    CAS

    Product licence number
         Cyclogest Pessaries 200mg      2343/0001
         Cyclogest Pessaries 400mg      2343/0002
         Depo-Provera 150mg/ml          0032/0082
         Depostat 200mg in 2ml          0053/0190
         Duphaston/Duphaston HRT        0512/5004R
         Farlutal 100mg tablets         3433/0056
         Farlutal 250mg tablets         3433/0058
         Farlutal 500mg tablets         3433/0080
         Farlutal 200mg/ml, 2.5ml       3433/0045
         Farlutal 200mg/ml, 5ml         3433/0045
         Femulen 500mcg                 08821/0015
         Gestone 25mg                   3194/0061
         Gestone 50mg                   3194/0062
         Gestone 100mg                  3194/0063
         Megace 40mg tablets            0125/0144
         Megace 160mg tablets           0125/0173
         Menzol 5mg tablets
         Micronor Oral Contraceptives   0242/0234
         Micronor HRT                   0242/0241
         Microval                       0011/0040
         Mirena                         0484/0025
         Neogest                        0053/0062
         Norgeston                      0053/0068
         Noriday                        088210036
         Noristerat                     0053/0095
         Norplant                       0109/0249
         Primolut N                     0053/5033R
         Provera 2.5mg                  0032/0168
         Provera 5mg                    0032/5035R

         Provera 10mg                   0032/0151
         Provera 100mg                  0032/0111
         Provera 200mg                  0032/0112
         Provera 400mg                  0032/0131
         Proluten Depot 250mg           0053/5031R
         Proluten Depot 500mg           0053/5032R

    MANUFACTURER

         Bristol-Myers Squibb
         Pharmaceuticals Ltd
         141-149 Staines Rd
         Hounslow
         Middlesex
         TW3 3JA
         0181 5727422

         Ferring Pharmaceuticals Ltd
         Greville House
         Hatton Road
         Feltham
         Middlesex
         TW14 9PX
         0181 8931543

         Hoechst Rousell Ltd
         Broadwater Park
         Denham
         Uxbridge
         Middlesex
         UB9 5HP
         01895 834343

         Janssen-Cilag Ltd
         PO Box 79,
         Saunderton,
         High Wycombe,
         Bucks
         HP14 4HJ
         01494 567567

         Organon Laboratories Ltd
         Cambridge Science Park,
         Milton Road,
         Cambridge
         CB4 4FL
         01223 423445

         Ortho
         see Janssen-Cilag

         P-D
         Parke-Davis Medical,
         Lambert Court,
         Chestnut Avenue,
         Eastleigh,
         Hants
         SO53 3ZQ
         01703 620500

         Pharmacia-Leiras Ltd
         Pharmacia & Upjohn
         Davy Avenue
         Knowlhill
         Milton Keynes
         MK5 8PH
         01908 661101

         Roussell
         see Hoechst-Roussell

         Schering Health Care Ltd
         The Brow,
         Burgess Hill,
         West Sussex
         RH15 9NE
         01444 232323

         Schwarz Pharma Ltd
         Schwarz House
         East Street
         Chesham
         Bucks
         HP5 1DG
         01494 772071

         Searle Pharmaceuticals
         PO Box 53,
         Lane End Road,
         High Wycombe,
         Bucks
         HP12 4HL
         01494 521124

         Solvay Healthcare Ltd
         Hamilton House
         Gaters Hill
         West End
         Southampton
         SO18 3JD
         01703 472281

         Upjohn Ltd
         See Pharmacia-Upjohn

         Wyeth Laboratories
         Huntercombe Lane South,
         Taplow,
         Maidenhead,
         Berks
         SL6 0PH
         01628 604377

    PRESENTATION

    Form

         Cyclogest Pessaries 200mg          pessaries
         Cyclogest Pessaries 400mg          pessaries
         Depo-Provera 150mg/1ml, 3.3ml      injection
         Depostat100mg/ml, 2ml              injection
         Duphaston/Duphaston HRT 10mg       tablets
         Farlutal 100mg,250mg, 500mg        tablets
         Farlutal 200mg/ml, 2.5ml & 5ml     injection
         Femulen 5mg                        tablets
         Gestone 25mg                       injection
         Gestone 50mg                       injection
         Gestone 100mg                      injection
         Megace 40mg, 160mg                 tablets
         Menzol 5mg                         tablets
         Micronor Oral Contraceptives       tablets
         Micronor HRT                       tablets
         Microval 30mcg                     tablets
         Mirena 20mcg/24hours               intra-uterine system
         Neogest 75mcg                      tablets
         Norgeston 30 mcg                   tablets
         Noriday 350mcg                     tablets
         Noristerat 200mg/ml                injection
         Norplant 38mg                      implant capsule
         Primolut N 5mg                     tablets
         Provera 2.5mg                      tablets
         Provera 5mg                        tablets
         Provera 10mg                       tablets
         Provera 100mg                      tablets
         Provera 200mg                      tablets
         Provera 400mg                      tablets
         Proluten Depot 250mg               injection
         Proluten Depot 500mg               injection
         Utovlan 5mg                        tablets

    Pack sizes

         Cyclogest Pessaries 200mg          - 15
         Cyclogest Pessaries 400mg          - 15
         Depostat                           - 1
         Depo-Provera 150mg, 3.3ml          - 1
         Depostat                           - 1
         Duphaston                          - 60
         Duphaston HRT                      - 42
         Farlutal 100mg tablets             - 20; 50
         Farlutal 500mg tablets             - 56
         Farlutal 200mg/ml, 2.5ml           - 1
         Farlutal 200mg/ml, 5ml             - 1
         Femulen                            - 28
         Gestone 25mg                       - 1
         Gestone 50mg                       - 1
         Gestone 100mg                      - 1
         Megace 40mg                        - 20
         Megace 160mg                       - 30
         Menzol                             - 3 x 24; 3 x60
         Micronor Oral Contraceptives       - 3 x 28
         Micronor HRT                       - 3 x 12
         Microval                           - 35
         Mirena                             - 1
         Neogest                            - 35
         Norgeston                          - 35
         Noriday                            - 3 x 28
         Noristerat                         - 1
         Norplant                           - 6 implants
         Primolut N                         - 30
         Provera 2.5mg                      - 30
         Provera 5mg                        - 10
         Provera 10mg                       - 10; 90
         Provera 100mg                      - 60
         Provera 200mg                      - 30
         Provera 400mg                      - 30
         Proluten Depot 250mg               - 1
         Proluten Depot 500mg               - 1

    PHYSIOCHEMICAL PROPERTIES

    Chemical structure

         Dydrogesterone - 6-Dehydro-9ß,10alpha-progesterone

         Ethynodiol acetate - 19-Nor-17alpha-pregn-4-en-20-yne-3ß

         Gestronol - NIF

         Hydroxyprogesterone hexanoate - 17alpha-Hydroxypregn-4-ene-3,20-
         dione hexanoate

         Levonorgestrel - 13-Ethyl-17ß-hydroxy-18,19-dinor-17alpha-pregn-
         4-en-20-yn-3-one

         Medroxyprogesterone acetate - 17alpha-Hydroxy-6alpha-methylpregn-
         4-ene-3,20-dione acetate

         Megestrol Acetate - 6-Methyl-3,20-dioxopregna-4,6-dien-17alpha-yl
         acetate

         Norgestrel - (±)-13-Ethyl-17ß-hydroxy-18,19-dinor-17alpha-pregn-
         4-en-20-yn-3-one

         Norethisterone - 17alpha-Ethinyl-19-nortestosterone, 17ß-hydroxy-
         19-nor-17alpha-pregn-4-en-20-yn-3-one, 17alpha-ethinyl-17ß-
         hydroxy-19-nor-androst-4-en-3-one

         Progesterone - Pregn-4-ene-3,20-dione

    Physical structure at room temperature

         All are solid

    Colour

         Dydrogesterone - white to pale yellow

         Ethynodiol acetate - white or almost white

         Gestronol - NIF

         Hydroxyprogesterone hexanoate - white or creamy white

         Levonorgestrel - white or almost white

         Megestrol Acetate - white or creamy-white

         Medroxyprogesterone acetate - white or off-white

         Norgestrel - white or almost white

         Norethisterone - white or yellowish-white

         Progesterone - white or slightly yellowish-white

    Odour

         Dydrogesterone - odourless or almost odourless

         Ethynodiol acetate - odourless or almost odourless

         Gestronol - NIF

         Hydroxyprogesterone hexanoate - odourless or almost odourless

         Levonorgestrel - odourless

         Megestrol Acetate - odourless or almost odourless

         Medroxyprogesterone acetate - odourless

         Norgestrel - almost odourless

         Norethisterone - odourless

         Progesterone - odourless

    Viscosity

         NA

    pH

         NA

    Solubility

    Dydrogesterone - Practically insoluble in water; soluble 1 in 40 of
    alcohol, 1 in 2 of chloroform, and 1 in 200 of ether; soluble in
    acetone; sparingly soluble in methyl alcohol; slightly soluble in
    fixed oils

    Ethynodiol acetate - very slightly soluble to practically insoluble in
    water; soluble in alcohol; freely to very soluble in chloroform;
    freely soluble in ether; sparingly soluble in fixed oils

    Gestronol - NIF

    Hydroxyprogesterone hexanoate - practically insoluble in water; freely
    soluble in alcohol and ether; very soluble in chloroform; dissolves in
    fixed oils and esters

    Levonorgestrel - practically insoluble in water; slightly soluble in
    alcohol, in acetone and in ether; soluble in chloroform; sparingly
    soluble in methylene chloride.

    Megestrol Acetate - practically insoluble in water; sparingly soluble
    in alcohol; very soluble in chloroform; soluble in acetone; slightly
    soluble in ether and in fixed oils.

    Medroxyprogesterone acetate - practically insoluble in water;
    sparingly soluble in alcohol and in methylalcohol; slightly soluble in
    ether; freely soluble in chloroform; soluble in acetone and dioxan

    Norgestrel - practically insoluble in water; the BP states that it is
    slightly, and the USP that it is sparingly soluble in alcohol;
    sparingly soluble in methylene chloride; freely soluble in chloroform

    Norethisterone - practically insoluble in water; slight to sparingly
    soluble in alcohol; soluble in chloroform and in dioxan; slightly
    soluble in ether.

    Progesterone - BP solublities are: practically insoluble in water;
    freely soluble in dehydrated alcohol; very soluble in chloroform;
    sparingly soluble in acetone, in ether and in fixed oils. USP
    solubilities are: practically insoluble in water; soluble in alcohol,
    in acetone and in dioxan; sparingly soluble in vegetable oils

    USES

    Indications

    To prevent conception; as part of hormone replacement regimes; as a
    hormone antagonist in malignant disease.

    Therapeutic Dose

    Contraceptive: 1 tablet (of whichever preparation prescribed) daily at
    the same time each day, starting on 1st day of cycle then
    continuously.

    Dydrogesterone - Endometriosis, 10mg 2-3 times daily from 5th to 25th
    day of cycle or continuously; Infertility, irregular cycles, 10mg
    twice daily from 11th to 25th day for at least 6 cycles (but not
    recommended); Habitual abortion, 10mg twice daily from day 11 to day
    25 of cycle until conception, then continuously until 20th week of
    pregnancy and gradually reduced; Dysfunctional uterine bleeding, 10mg
    twice daily (together with an oestrogen) for 5-7 days to arrest
    bleeding; 10mg twice daily (together with an oestrogen) from 11th to
    25th day of cycle to prevent bleeding; Dysmenorrhoea, 10mg twice daily
    from 5th to 25th day of cycle; Amenorrhoea, 10mg twice daily form 11th
    to 25th day of cycle with oestrogen therapy from 1st to 25th day of
    cycle; Pre-menstrual syndrome, 10mg twice daily from 12th to 26th day
    of cycle, increased if necessary (but not recommended); HRT, 10mg
    daily on days 15-28 of each 28-day oestrogen HRT cycle, increased to
    10mg twice daily if withdrawal bleed is early or endometrial biopsy
    shows inadequate progestational response.

    Hydroxyprogesterone hexanoate - Habitual abortion, 250-500mg weekly by
    slow intra-muscular injection during first half of pregnancy.

    Medroxyprogesterone acetate - Dysfunctional uterine bleeding, 2.5-10mg
    daily for 5-10 days beginning on 16th-21st day of cycle, repeated for
    2 cycles, for secondary amenorrhoea repeat for 3 cycles; Mild to
    moderate endometriosis, 10mg 3 times daily for 90 consecutive days,
    beginning on 1st day of cycle; Endometrial, prostate and renal cancer,
    100-500mg daily; Breast cancer, various doses in range 0.4-1.5g daily;

    by deep intramuscular injection for malignant disease, various doses
    in range 1g daily down to 250mg weekly.

    Megestrol Acetate - Breast cancer, 160mg daily in single or divided
    doses; endometrial cancer, 40-320mg daily in divided doses.

    Norethisterone - Endometriosis, 10mg daily starting on 5th day of
    cycle (increased if spotting occurs to 20-25mg daily, reduced once
    bleeding has stopped); Menorrhagia, 5mg 3 times daily for 10 days to
    arrest bleeding; to prevent bleeding 5mg twice daily from 19th to 26th
    day; Dysmenorrhoea, 5mg 3 times daily from 5th to 24th day for 3-4
    cycles; Pre-menstrual syndrome, 5mg 2-3 times daily from 19th to 26th
    day for several cycles (but not recommended); Postponement of
    menstruation, 5mg three times daily starting 3 days before anticipated
    onset (menstruation occurs 2-3 days after stopping); HRT 1mg daily on
    days 15-26 of each 28-day oestrogen HRT cycle; Breast cancer, 40mg
    daily, increased to 60mg daily if required.

    Progesterone - Pre-menstrual syndrome, pessaries - 200mg daily to
    400mg twice daily starting on day 12-14 and continued until onset of
    menstruation (but not recommended); rectally if barrier methods of
    contraception are used, or if vaginal infection; Embryo transfer, deep
    intramuscular injection as per data sheet.

    Contraindications

    Pregnancy (except where licensed);a history during pregnancy of
    idiopathic jaundice or severe pruritis. Acute or severe chronic liver
    diseases including liver tumours. Dubin-Johnson or Rotor syndrome.
    Undiagnosed abnormal vaginal bleeding. Thrombo-embolic disorders,
    thrombophlebitis, cerebrovascular disorders, coronary artery disease,
    myocardial infarction, angina, hyperlipidaemia or a history of these
    conditions.

    Abuses

         NIF

    HAZARD/RISK CLASSIFICATION

         NIF

    PHARMACOKINETICS

    Absorption

    Dydrogesterone
         NIF

    Ethynodiol acetate
         almost 100%

    Gestronol
         NIF

    Hydroxyprogesterone hexanoate
         90%

    Megestrol Acetate
         about 100%

    Medroxyprogesterone acetate
         <100%

    Norgestrel
         NIF

    Norethisterone
         100%

    Progesterone - extensive

    Distribution

    Dydrogesterone
         NIF

    Ethynodiol acetate
         33l - extensively bound to albumin and more specifically to sex
         hormone binding globulin

    Gestronol
         NIF

    Hydroxyprogesterone hexanoate
         5l

    Levonorgestrel
         93-95% plasma bound

    Megestrol Acetate
         NIF

    Medroxyprogesterone acetate
         >20l, 94% is protein bound

    Norethisterone
         95% plasma bound

    Norgestimate
         NIF

    Norgestrel
         NIF

    Progesterone
         17-29l, 95-98% plasma protein bound

    Metabolism

    Dydrogesterone
         Metabolised to glucuronide conjugates

    Ethynodiol acetate
         Metabolised in liver or gut wall to norethisterone and then to
         sulphate and glucuronide conjugates.

    Gestronol
         NIF

    Hydroxyprogesterone hexanoate
         metabolised in liver

    Levonorgestrel
         Extensively metabolised by the liver

    Megestrol Acetate
         metabolised by liver to glucuronide conjugates

    Medroxyprogesterone acetate
         extensively metabolised in the liver

    Norgestimate
         NIF

    Norgestrel
         NIF

    Norethisterone
         Metabolised in the intestinal wall and liver

    Progesterone
         About 75% is metabolised presystemically to glucuronide
         conjugates by the liver

    Elimination

    Dydrogesterone
         60% is excreted via the urine within 72 hours. Only small amounts
         are excreted via the faeces

    Ethynodiol acetate
         via urine and faeces

    Gestronol
         NIF

    Hydroxyprogesterone hexanoate
         NIF

    Levonorgestrel
         20-30% eliminated via the faeces and the rest via the urine

    Megestrol Acetate
         excreted as metabolites via the urine and faeces

    Medroxyprogesterone acetate
         mainly as conjugated metabolites in the faeces

    Norethisterone
         60% as metabolites in urine and faeces

    Norgestrel
         NIF

    Progesterone
         mainly as conjugates in the urine

    Half-life

    Dydrogesterone
         about 6h

    Ethynodiol acetate
         about 25h

    Gestronol
         NIF

    Hydroxyprogesterone hexanoate
         2-11h, mean 4h

    Levonorgestrel
         10.26h

    Megestrol Acetate
         15-20h

    Medroxyprogesterone acetate
         about 30h

    Norgestrel
         NIF

    Norethisterone
         5 -12h

    Progesterone
         distribution - 3-6min; elimination - 19-95min

    Breast Milk

    Dydrogesterone
         small quantities are have been measured in breast milk, but this
         is unlikely to present any risk to the infant

    Ethynodiol acetate
         norethisterone concentration appears to reach a peak at about
         4-8h after ingestion of ethynodiol acetate, small amounts of
         norethisterone are excreted into breast milk, the concentration
         being 10-20% of that in plasma

    Gestronol
         NIF, contraindicated in lactation

    Hydroxyprogesterone hexanoate
         contraindicated in lactation

    Levonorgestrel
         Approximately 0.1% of the daily dose passes into breast milk

    Megestrol Acetate
         Disease states being treated would usually contraindicate
         breast-feeding

    Medroxyprogesterone acetate
         excreted into breast milk in concentrations similar to those in
         plasma. No special precautions are advised.

    Norgestrel
         NIF

    Norethisterone
         daily oral dose of 350micrograms for contraception were reported
         in one study to reduce milk volume somewhat but do not usually
         affect volume or composition. Intramuscular injections of 200mg
         each 8 weeks do not interfere with lactation. The plasma/milk
         ratio of the heptanoate is about 10 and only 0.1% of the dose,
         estimated as a maximum of 1.5micrograms daily, reaches the baby.
         this is unlikely to affect the bay and is undetectable in the
         baby's plasma at the time of the peak maternal plasma level.
         There is a theoretical risk of all steroids interfering with
         bilirubin conjugation, and maternal use of norethisterone should
         probably be avoided whilst a baby has neonatal jaundice.

    Progesterone
         excreted in low concentrations, which are unlikely to have any
         effect on the infant

    TOXICOKINETICS

         NIF

    EPIDEMIOLOGY OF POISONING

    In 1994, 2007 calls were made to UK NPIS centres about hormonal
    contraceptive poisoning.

    ADVERSE EFFECTS

    General - Headaches/migraine, nausea, vomiting, breast changes, change
    in weight, changes in libido, chloasma, breakthrough bleeding and
    spotting, rash, depression, irregular cycle length, ocular changes,
    increase in size uterine myofibromata and changes in carbohydrate,
    lipid or vitamin metabolism. Rarely dizziness, hirsutism, haemorrhagic
    eruption and colitis have been reported in users of progestogen-only
    oral contraceptives

    Megesterol - as above, rare reports of dyspnoea, heart failure,
    hypertension, hot flushes, mood changes, cushingoid faces, tumour
    flare (with or without hypercalcaemia), hyperglycaemia, alopecia and
    carpel tunnel syndrome. Prolonged administration may cause  urticaria.
    Clinical and laboratory evidence of mild adrenal suppression

    INTERACTIONS

    Metabolism accelerated by rifamycins; increased plasma-cyclosporin
    levels (inhibition of metabolism); aminoglutethimide reduces plasma
    concentration of medroxyprogesterone

    MECHANISM OF ACTION

    Progestogens are synthetic compounds with actions similar to that of
    progesterone. Progesterone is the main hormone secreted by the corpus
    luteum. Large quantities are produced by the placenta during
    pregnancy. It acts on the endometrium by converting the proliferative
    phase induced by oestrogen to a secretory phase and preparing the
    uterus to receive the fertilised ovum.

    FEATURES OF POISONING

    Acute

    Ingestion

    Toxicity is unlikely following an acute overdose. Occasionally there
    may be nausea and vomiting. Withdrawal bleding may occur in females
    even in pre-pubertal girls.

    Chronic

    Ingestion/Injection

    Chronic or high dose therapy can result in jaundice, headache,
    dizziness, oligomenorrhea or amenorrhea, congestion of the breasts and
    decreased libido. Chronic toxicity may produce a thromboembolic state.

    Pregnancy

    During the pre-embryonic phase, which lasts until 17 days
    post-conception, the 'all or nothing' concept is thought to apply.
    During this period, cells damaged by a toxic insult, such as a drug
    exposure, will be replaced by extra divisions of the remaining cells
    which will then develop normally. If extensive damage occurs, failure
    of implantation and spontaneous abortion may occur. Thus, if the
    pregnancy is maintained, the risks to the fetus are likely to be no
    greater than those for the general population.

    The maternal administration of norethisterone to several species of
    animals, including non-human primates, caused masculinisation of the
    external female genitalia of the offspring but did not increase the
    incidence of non-genital adverse fetal effects.1

    There is no conclusive evidence of an association between progestogen
    exposure in early pregnancy and non-genital malformations. Androgenic
    hormones in human pregnancy have been associated with a small risk of
    genital abnormalities when exposure occurs around about 6-7 weeks of
    gestational age when the genitalia are beginning to develop.1-4
    Approximately 1% of female fetuses exposed at this critical period of
    development develop genital anomalies e.g. enlarged clitoris and
    labial folds1,4. Internal genitalia and subsequent pubertal
    development are not affected by norethisterone taken during pregnancy.
    Male infants have an even smaller risk of genital anomalies, usually
    hypospadias which can be treated surgically.

    However, a recent meta-analysis of 14 studies involving 65,567 women
    concluded that there was no association between 1st trimester exposure
    to sex hormones generally, or to oral contraceptives specifically, and
    external genital malformations.5

    The use of norethisterone during any stage of pregnancy is
    contra-indicated.

    A number of congenital malformations, including cardiovascular,
    central nervous system, multiple organ and limb defects, have been
    reported in infants exposed to the drug  in utero.1,2,3,4 However, the
    role of norethisterone in the development of these anomalies has not
    been established due to the influence of other factors such as alcohol
    ingestion, cigarette smoking, concomitant drug therapy and maternal
    obstetric history.1,3

    There are three prospective follow-up reports from the European
    Network of Teratology Information Services (ENTIS) following exposure
    to progestogens during pregnancy. One patient had Norplant removed
    after conception (details of timing of exposure not available), a
    normal full term infant was born; there were two reports of exposure
    to Depo-Provera, one woman had a dose at 1 week and 12 weeks of
    gestation, a normal fullterm infant was born, the second woman was
    exposed at 5 weeks of gestation and had an elective termination.

    References

    1. Gilstrap III LC, Little BB. Drugs and Pregnancy. Amsterdam:
    Elsevier Science Publishing, 1992: 242-244

    2. Folb PI, Dukes MNG (Eds). Drug Safety in Pregnancy. Amsterdam:
    Elsevier Science Publishing, 1990: 273-281

    3. Briggs CG, Freeman RK, Yaffe SJ. Drugs in Pregnancy and Lactation.
    4th ed. Baltimore: Williams and Wilkins, 1994

    4. Schardein JL. Chemically Induced Birth Defects. 2nd ed. New York:
    Marcel Dekker, 1993

    5. Raman-Wilms L et al. Obs Gyn 1995; 85: 141-9

    MANAGEMENT

    Symptomatic treatment only is required.
    Parents of prepubertal girls should be warned of the possibility of a
    withdrawal bleed several days after ingestion.

    ANALYSIS

         NIF

    PREVENTION OF POISONING

         NIF

    OTHER TOXICOLOGICAL DATA

    Carcinogenicity

    In a retrospective study of 5000 black women who received depot
    medroxyprogesterone for contraception, no increased incidence in
    breast, ovarian, or uterine corpus cancer was seen up to 13 years
    later. (Liang et al 1993).
    There is considerable evidence suggesting that after induction by
    chemical carcinogens, sex hormones act as promoters of
    heptocarcinogenesis.

    Teratogenicity

    There is no conclusive evidence of an association between progestogen
    exposure in early pregnancy and non-genital malformations. Exposed
    female infant have a small risk (approximately 1%) of clitoral
    hypertrophy and fusion of the labioscrotal folds, when exposure occurs
    during the critical period of genital development. These anomalies can
    be corrected surgically. Male infants have an even smaller risk of
    genital anomalies, usually hypospadias which can be treated
    surgically.

    Author

    Helen Seymour, BPharm (Hons)

    National Poisons Information Service (Newcastle Centre)
    Regional Drug & Therapeutics Centre
    Wolfson Building
    Claremont Place
    Newcastle upon Tyne
    NE1 4LP
    UK

    This monograph was produced by the staff of the Newcastle Centre of
    the National Poisons Information Service in the United Kingdom. The
    work was commissioned and funded by the UK Departments of Health, and
    was designed as a source of detailed information for use by poisons
    information centres.

    Peer review was undertaken by the Directors of the UK National Poisons
    Information Service.

    Last updated January 1997

    REFERENCES

    1. Martindale: The Extra Pharmacopoeia. 31st Edition. Reynolds JEF
    (Ed.). Pharmaceutical Press 1996.

    2. Therapeutic Drugs. Dollery C. (Ed.). Churchill Livingstone 1991.

    3. ABPI Compendium of Data Sheets and Summaries of Product
    Characteristics. Datapharm Publications Ltd. 1996-97.

    4. British National Formulary. Number 32 (September 1996). British
    Medical Association and Royal Pharmaceutical Society.

    5. Poisindex Systemœ, Micromedex, Inc., Denver Colorado, Edition
    Expires 31.12.96.

    6. National Teratology Information Service.

    7. European Commission; Poison centres: Collection of the annual
    reports 1994, Analysis and synthesis, Final Report 31.8.96.