Pharma Flashcards

1
Q

Which groups of drugs cause hyperproloactinaemia?

A

SSRIs
Metoclopramide
Oestrogens
Opioids
H2 antagonists (Cimetidine)
Calcium channel blockers

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2
Q

Which progesterones are associated with high risk of VTE, when used as part of COCP?

A

VTE risk per 10,000 women per year

None (not pregnant) 1-2

Ethinylestradiol plus
Levonorgestrel (eg Microgynon, Rigevidon) OR
Norgestimate (eg Cilest) OR
Norethisterone (eg Loestrin, Norimin)

5-7

Ethinylestradiol plus
Gestodene (eg Femodette) OR
Desogestrel (eg Mercilon) OR
Drospirenone (eg Yasmin)

9-12

Pregnancy 10/10,000

Ethinylestradiol plus
Etonogestrel (Nuvaring) OR
Norelgestromin (Evra)

6-12

Ethinylestradiol plus
Cyproterone acetate (Dianette)

limited data approx 9-12

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3
Q

How do anticholinergic drugs work?

A

Anticholinergic drugs act by blocking muscarinic receptors in the bladder smooth muscle, leading to a direct relaxant effect.
(Bladder is M3 specifically)

Side effects: dry mouth, constipation and dry eyes occur as a result of blockade of these receptors at other sites.

Contraindications: Myasthenia gravis, significant bladder outflow obstruction, severe ulcerative colitis, toxic megacolon and in gastrointestinal obstruction or atony.
May aggravate prostatic hypertrophy and congestive cardiac failure

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4
Q

What are the mechanisms of action of emergency contraception?

A

3 types

  • Levonelle (Levenogestrel)
    Synthetic progesterone
    1.5mg
    Upto 72 hours from intercourse

EllaOne (Ullipristal)
Progesterone modulator
30mg
Upto 72 hours from intercourse

Contraindicated severe asthma or liver impairment

Copper IUD
Upto 7 days from intercourse

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5
Q

What is the mechanism of action of Desmopressin/DDAVP?

A

DDAVP is synthetic version of Vasopressin
Increases factor VIII and VWF by 3-4x
No impact of factor IX

Exerts action through V2 receptors on Endothelial cells
Uterus expresses V1 receipts - safe in pregnancy

Dose is 0.3 micrograms/kg of prepregnancy weight
Repeat doses can be given 12-24 hourly although may be less effective

Beware risk of hyponatremia - need to fluid restrict when giving
Don’t give to those on diuretics

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6
Q

What is the impact of anti-TNF drugs when used in pregnancy?

A

No difference in rate of fetal malformations

Concerns that anti-TNF accumulates in the neonate as transplacental transfer increases in later stages of pregnancy
To avoid neonatal immunosuppression it is recommended anti-TNF drugs are stopped in pregnancy as below:

All are safe with breastfeeding
Infliximab Stop at 16 weeks gestation
Etanercept Stop prior to third trimester
Adalimumab Stop prior to third trimester
Certolizumab Safe all trimesters

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7
Q

What is the dose of MgS04? for hypertension or neuroprotection?

A

A loading dose of 4 g should be given intravenously over 5 to 15 minutes, followed by an infusion of 1 g/hour maintained for 24 hours. If the woman has had an eclamptic fit, the infusion should be continued for 24 hours after the last fit.

Recurrent fits should be treated with a further dose of 2 g to 4 g given intravenously over 5 to 15 minutes

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8
Q

What is the MOA of Terbutaline?

A

Selective beta-2 adrenergic receptor agonist

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9
Q

What is the role of anti-D following transfusion of blood products?

A

Platelets - up to 5 pools 1 x 250 micrograms Anti D IM
Red blood cells: 1 unit - 1500 or 2500 IG Anti-D
More than 1 unit - Red blood cell exchange transfusion

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10
Q

What is the maximum dosage of lidocaine in pregnancy?

A

Max dose is 3mg/kg (7mg/kg with adrenaline)

Blocks fast voltage gated sodium channels
Anti-arrhythmic
Half life 2 hours
Safe to use in pregnancy
Hepatic metabolism

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11
Q

Which anti epileptic drugs are enzyme inducing and non enzyme inducing?

A

ENZYME INDUCING:
carbamazepine
phenytoin
phenobarbital
primidone
oxcarbazepine
topiramate
eslicarbazepine

Avoid COCP/Patch/ring/POP/implant for contraception

NON ENZYME INDUCING:
sodium valproate
levetiracetam
gabapentin
vigabatrin
tiagabine
pregabalin

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12
Q

What consideration should be taken about contraception if a woman is taking lamotrigine?

A

Women taking lamotrigine and oestrogen-containing contraceptives should be informed of the potential increase in seizures due to a fall in the levels of lamotrigine.

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13
Q

In which patients is Cabergoline contraindicated?

A

Cabergoline - dopamine agonist
Used to stop lactation

Contraindicated in:
Pre-eclampsia
Cardiac valvulopathy (exclude before treatment)
History of pericardial fibrotic disorders
History of puerperal psychosis
History of pulmonary fibrotic disorders
History of retroperitoneal fibrotic disorders

Hypersensitivity to ERGOT ALKALOIDS

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14
Q

What drugs can be used to treat uncomplicated falciparum malaria?

A

Treatment options for uncomplicated falciparum are:

Oral quinine 600 mg 8 hourly and oral clindamycin 450 mg 8 hourly for 7 days OR
Artemether and Lumefantrine (Riamet®) 4 tablets/dose for weight > 35 kg, twice daily for 3 days
OR
Atovaquone-proguanil (Malarone®) 4 standard tablets daily for 3 days

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15
Q

Describe fetal anomalies associated with antiepileptic drugs

A

Phenytoin:
Fetal hydantion syndrome
Includes: heart defects, cleft lip or palate, skeletal malformations, and microcephaly.

Minor malformations, including strabismus, hypertelorism, distal digital hypoplasia, nail hypoplasia, clubfoot, and abnormal dermatoglyphic patterns.

Coagulopathy occurs in ~50% of babies born to mothers on phenytoin - deficiency of vitamin K dependent clotting factors - very few of these babies are symptomatic.

Phenobarbital:
Associated with minor anomalies as with phenytoin. Exposed infants can have barbiturate depression or drug withdrawal at birth

Carbamazepine:
Associated with neural tube defects (~1% risk compared to ~0.1% background risk). Exposure to carbamazepine after the neural tube has closed (days 22-29) does not produce this defect.

Valproic acid:
RISK OF NTD FROM 6 in 10,000 to 100 to 200 in 10,000.
Associated with neural tube defects (1-2% risk) and is specific for spina-bifida, not anencephaly.
Patients with higher serum levels of valproic acid may be at greatest risk because the majority of cases occur in infants exposed to more than 1,000 mg/day.

Sodium valproate also associated with polycystic ovaries

Lithium:
Increases the rate of fetal heart defects to around 60 in 1000, compared with the risk of 8 in 1000 in the general population.
It is estimated that lithium increases the risk of Ebstein’s anomaly (a major cardiac malformation) from 1 in 20,000 to 10 in 20,000.

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16
Q

What is the impact of the following immunosuppressive drugs on pregnancy/in utero?

Prednisolone
Azathioprine
Cyclosporin
Tacrolimus
Mycophenolate

A

PREDNISOLONE
Crosses the placenta but fetal concentrations are ~10% maternal concentrations.
Not teratogenic although cases of cleft palate have been reported.

AZATHIOPRINE
Metabolised in adults to 6-mecarptopurine.
Fetal liver lacks the enzyme for this conversion and the fetus is relatively protected.
Associated with low birth weight, prematurity, neonatal jaundice and respiratory distress

CYCLOSPORIN
Metabolism increases in pregnancy and higher doses may be required to maintain plasma levels.
Associated with low birth weight, maternal diabetes and hypertension

TACROLIMUS
Dose may have to be reduced by up to 60% to avoid toxicity.
This is due to inhibition of hepatic cytochrome P450 enzymes during pregnancy (responsible for tacrolimus metabolism).

Mycophenolate - teratogenic, not used in pregnancy

17
Q

Which SSRIs are not excreted in breast milk?

A

Paroxetine
Sertraline

18
Q

What is the MOA of Letrozole?

A

Aromatase inhibitor

19
Q

Which progestogen has anti-androgenic and anti-mineralocorticoid activity?

A

Drosperidone (4th generation progestogen)

20
Q

What type of receptor is Oestrogen?

A

Nuclear transciption receptor
It has alpha and beta subtypes

21
Q

Describe the impact of Tamoxifen on the breasts/ reproductive tract

A

Breasts

Antagonises oestrogen actions on breast
Adjuvant tamoxifen in women with breast cancer associated with a 50% reduction in recurrence and a 25% reduction in mortality.

Reproductive tract

Anti-oestrogenic effects in pre-menopausal women - can cause ovarian cysts/amenorrhoea

Oestrogenic effects in post-menopausal women with stimulation of the endometrium, myometrium and vagina. There is stimulation of fibroid growth, induction / re-activation of endometriosis and adenomyosis.

Use is associated with increased hepatic synthesis of sex hormone, thyroxine and cortisol binding globulins.
Free thyroxine and TSH levels are unchanged

22
Q

What is the MOA of Clomiphene Citrate?

A

Weak oestrogen, competes with endogenous oestrogens for receptors at the hypothalamus blocking negative feed-back of endogenous oestrogens

· GnRH levels rise and stimulate gonadotrophin release resulting in ovarian stimulation and rise in serum oestradiol

· Effective for ovulation induction in women with anovulatory infertility

· 5-10% risk of multiple pregnancy, risk of ovarian hyper-stimulation

· Side-effects include visual disturbance (discontinue therapy), hot flushes, abdominal discomfort, breast tenderness, menorrhagia, dizziness, hair loss, weight gain, rash, insomnia and depression

23
Q

What is the mechanism of action of cytotoxic chemotherapy agents?

Platinum based
Anti-microtubule
Anthracyclines
Topoisomerase Inhibitor
Anti-metabolite
Anti-tumour

A

Platinum based (Carboplatin or Cisplatin) - form DNA adducts, which insert in place of nucleosides causing error in DNA replication
Carboplatin (with Paclitaxel) used for epithelial ovarian, fallopian tube and primary peritoneal cancers
Cisplatin used with radiotherapy (which sensitises tissue) in cervical, vulval, vaginal cancers

Anti-microtubule (Paclitaxel or Docetaxel) - Prevent the microtubule from separating (depolymerisation) during cell division

Anthracyclines (Doxorubicin) - Intercalate into DNA structure and inhibit DNA, RNA, protein synthesis. Inhibit topoisomerase II enzyme, (stops DNA replication), induce free radical production
Most gonadotoxic - “Red Devil”
Used in platinum resistant cancers

Topoismerase inhibitor (Topotecan, Etoposide) - inhibits enzyme Topoisomerase enzyme that allows uncoiling of DNA for replication

Anti-metabolite (Gemcitabine) - mimics nucleotide base cytosine, stopping replication and inhibits ribonucelotide reductase which synthesis deoxynucelosides for DNA replication

Anti-tumour (bleomycin) - forms activated complex in presence of O2 and metal ions which causes free radicals
BEP regimen (Bleomycin, Etoposide, Cisplatin) used in gynaecology to treat germ cell tumours of the ovary

24
Q

What is the mechanism of action of
Tamoxifen
Letrozole

A

Tamoxifen is a oestrogen receptor modulator - alters the shape of the receptor and presents estradiol from binding to it

Letrozole/Anastrazole is an Aromatase inhibitor - competitively inhibit aromatase + therefore reduce circulating levels of oestrogen

25
Q

What considerations should be taken if a HIV positive woman conceives on Dolutegravir?

A

A woman planning a pregnancy and/or conceiving on dolutegravir should be seen as soon as possible to discuss current evidence on neural tube defects

Women taking dolutegravir who are trying to conceive should be recommended to take folic acid 5 mg od

26
Q

What is the MOA of Mifepristone?

A

Progesterone antagonist

Derivative of norethindrone (19-norsteroid) - similar chemical structure to progesterone / glucocorticoids.

Progesterone / glucocorticoid antagonist.

Like progesterone, binds to the progesterone receptor causing dimerisation of the receptor and binding to progesterone response elements of progesterone responsive genes. Unlike progesterone, however, transcription is inhibited.

27
Q

What is the treatment of thrush and recurrent thrush in the pregnant and non-pregnant population?

A

THRUSH
Non-pregnant
Fluconazole 150mg STAT
or Clotrimazole pessary 500mg STAT

Pregnant
Clotrimazole pessaries 500mg OD 7/7

RECURRENT THRUSH
Non-pregnant
Fluconazole 150mg every 72 hours for 3 doses
then once weekly induction regimen

Pregnant
Clotrimazole 500mg OD 10-14 days then weekly maintenance
Maintenance length is for 6 months for both

If Azole resistant - then Nystain 100,00 units per vagina 12-14 nights initially or14 nights/month as maintenance if recurrent