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P1EXAM > Original Pharmacology > Flashcards

Original Pharmacology Flashcards

1
Q

What do strong opioids act as?

A

Mu receptors agonists

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2
Q

What do weak opioids act as?

A

Mu, delta or kappa receptor agonists

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3
Q

What are the features of warfarin embryopathy?

A

Hypoplasia of nasal bridge
Congenital heart defects
Ventriculomegaly
Agenesis of the corpus callosum
Stippled epiphyses

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4
Q

What proportion of exposed fetuses develop warfarin embryopathy?

A

5%

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5
Q

At what gestation may warfarin embryopathy occur?

A

6-12 weeks

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6
Q

How does warfarin work?

A

Inhibits vitamin K dependent clotting factors - 10,9,7,2

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7
Q

Is warfarin safe to use in breastfeeding?

A

Yes

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8
Q

What should warfarin be switched for during pregnancy?

A

LMWH

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9
Q

What are the 2 most common dihydrofolate reductase (DHFR) inhibitors?

A

1) Methotrexate
2) Trimethoprim

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10
Q

What is the max dose of lidocaine?

A

3mg/kg (7mg/kg with adrenaline)

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11
Q

What is the lidocaine conversion?

A

1% lidocaine =1g/100mL or 10mg/mL

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12
Q

What is the half-life of lidocaine?

A

2 hours

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13
Q

What is the mechanism of action of lidocaine?

A

Blocks fast voltage gated sodium channels

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14
Q

What are the 2 different antenatal steroid courses available?

A

Betamethasone 12 mg IM x 2 doses or
Dexamethasone 6 mg IM x 4 doses

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15
Q

How many x more potent is fentanyl than morphine?

A

x80-100

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16
Q

What are the adverse effects of ACEi/ARBs on a fetus?

A

1) Congenital Malformations
2) Renal dysgenesis
3) Oligohydramnios as a result of fetal oliguria
4) Pulmonary hypoplasia
5) IUGR
6) Neonatal anuric renal failure

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17
Q

What are the adverse effects of carbimazole on a fetus?

A

1) Choanal atresia - narrowed nasal cavity
2) GIT defects
3) Omphalocoele
4) Aplasia cutis - localised absence of skin

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18
Q

What is the mode of action of cyclizine?

A

Histamine H1-receptor antagonist

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19
Q

What is the mode of action of promethazine?

A

Histamine H1-receptor antagonist

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20
Q

What is the mode of action of ondansetron?

A

Serotonin 5-HT3 receptor antagonist

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21
Q

What is the mode of action of prochlorperazine?

A

Dopamine D2 receptor antagonist

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22
Q

What is the mode of action of metoclopramide?

A

Dopamine D2 receptor antagonist
5-HT3 receptor antagonist
5-HT4 receptor agonist

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23
Q

In whom would you not consider metoclopramide in pregnancy and why?

A

In those <20 years old due to the risk of oculogyric crisis

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24
Q

When may warfarin be restarted after delivery?

A

5-7 days after - although it is safe in breastfeeding the delay is due to to the risk of PPH

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25
Q

What are the phase 1 reactions of drug metabolism?

A

Oxidation, reduction or hydrolysis —> leading to products being more reactive

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26
Q

What are the phase 2 reactions of drug metabolism?

A

Conjugation —> leading to inactivation of a drug

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27
Q

In those at risk of VTE, when should LMWH be started?

A

In the first trimester

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28
Q

How does heparin prevent coagulation?

A

Inactivation of antithrombin III

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29
Q

What are the S/Es of heparin?

A

1) Bleeding
2) Thombocytopenia
3) Hypoaldosteronism
4) Osteoporosis

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30
Q

What is the most common inherited haemostatic disorder?

A

Von Willebrand’s

A disorder leading to increased bleeding

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31
Q

What blood test profile represents Von Willebrand’s

A

PT = unaffected
APTT = prolonged
Bleeding time = prolonged
Plt count = unaffected

APTT links to intrinsic side

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32
Q

Which Abx damage the 8th cranial nerve in the fetus and are ototoxic?

A

The aminoglycosides - e.g. gentamicin and streptomicin

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33
Q

Which Abx can cause neonatal haemolysis?

A

Both sulphonamides and trimethoprim (an co-trimoxazole which is a combination of the two)

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34
Q

Which local anaesthetic(s) are amide?

A

Lidocaine

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35
Q

Which local anaesthetic(s) are ester?

A

Benzocaine; procaine; tetracaine

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36
Q

Which anti-hypertensive is an alpha-2-agonist?

A

Methyldopa

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37
Q

What is the half life of warfarin?

A

40 hours

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38
Q

How long does it take for warfarin to reach its full effect?

A

3 days

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39
Q

How does tranexamic acid work?

A

Inhibits the activation of plasminogen

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40
Q

Maternal use of metronidazole during breastfeeding is associated with what in the infant?

A

Diarrhoea

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41
Q

Over what period after administration are corticosteroids most effective in reducing respiratory distress if delivery occurs?

A

24 hours - 7 days

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42
Q

Through which mechanism of action and which receptor does cabergoline suppress lactation?

A

Dopamine agonist
At D2 receptor

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43
Q

What is the mechanism of action of clomifene?

A

Blocks oestrogen receptors in the hypothalamus, increasing FSH pulse frequency

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44
Q

What is the mechanism of action of mifepristone?

A

Progesterone antagonist

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45
Q

What type of drug is misoprostal?

A

Synthetic prostaglandin

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46
Q

What is the main estrogenic component of the combined oral contraceptive pill?

A

Ethinylestradiol

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47
Q

What class of drug is ulipristal acetate?

A

Selective progesterone receptor modulator

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48
Q

What is the mechanism of action of hydralazine?

A

Direct smooth muscle relaxant

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49
Q

Which enzyme is blocked by acetazolamide?

A

Carbonic anhydrase

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50
Q

What is the total extra iron requirement in pregnancy?

A

1000mg

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51
Q

What is the major constituent of pulmonary surfactant?

A

Dipalmitoylphosphatidylcholine

“dipal-mitoyl-phospha-tidyl-choline”

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52
Q

What are the S/Es of labetolol in pregnancy?

A

IUGR, with prolonged use

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53
Q

What are the S/Es of methyldopa?

A

1) Rebound HTN
2) Depressed mood
3) Flattened CTG variability
4) Hepatitis

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54
Q

What type of drug is nifedipine?

A

Dihydropyridine - it blocks inwards flux of calcium through voltage gated channels

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55
Q

What are the S/Es of nifedipine?

A

1) Acute hypotension
2) Peripheral oedema
3) Headache and flushing

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56
Q

What are the affects of ACEi’s in pregnancy?

A

1) Congential malformations, esp. to CVS
2) Skull defect
3) Oligohydramnios

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57
Q

What is the first line tocolytic?

A

Nifedipine

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58
Q

What is the 2nd line tocolytic?

A

Atosiban

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59
Q

What type of drug is atosiban?

A

Oxytocin antagonist

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60
Q

What drug may be given prior to ECV?

A

Terbutaline can increase procedural success in primips. It is a one-off dose and can cause S/Es of transient maternal tachycardia and tremor

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61
Q

Women at risk of pre-eclampsia and should be offered aspirin 75mg are:

A
  1. HTN during pregnancy / chronic
  2. CKD
  3. Autoimmune disease e.g. SLE
  4. T1DM or T2DM
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62
Q

What are the S/E of nitrous oxide?

A

Nausea

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63
Q

What are the S/Es of IM pethidine?

A

N+V
Narcosis
Respiratory depression in the neonate if given within 2 hours of delivery

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64
Q

In whom should carboprost be avoided?

A

Caution in HTN, avoided in asthma

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65
Q

In whom should ergometrine be avoided?

A

HTN

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66
Q

What are the potential side effects of epidural?

A

1) Hypotension
2) Loss of mobility
3) Higher chance of assisted delivery
4) Complications associated with insertion, e.g. dural tap, haematoma, high blockade

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67
Q

What may be used as an anti-emetic in resistant cases of HG where everything else have been tried?

A

Corticosteroids

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68
Q

Why is heartburn more common in pregnancy?

A

The action of progesterone on the lower oesophageal sphincter causes it to have reduced tone.

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69
Q

What is the mechanism of action of mefenamic acid?

A

Prostaglandin production inhibitor

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70
Q

By how much may mefenamic acid reduce bleeding?

A

30%

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71
Q

What is the mechanism of action of tranexamic acid?

A

Anti-fibrinolytic - blocks conversion of plasminogen to plasmin, reducing fibrinolysis

72
Q

By how much may tranexamic acid reduced blood loss?

A

40-50%

73
Q

What drugs may be used to reduce detrusor over-activity (urge incontinence)?

A

Tolterodine and oxybutynin - both are muscarinic antagonists on M3

74
Q

What drug might be used in stress incontinence?

A

Duloxetine - it increases urinary sphincter tone, SNRI action

75
Q

What are the different classes of cytotoxic agents?

A

1) Antimetabolites
2) Alkylating agents
3) Intercalating agents
4) Anti-tumour antibiotics
5) Drugs directed against spindle microtubules, inhibiting mitosis

76
Q

What are examples of antimetabolites?

A

5-FU, methotrexate

77
Q

What is an example of alkylating agents?

A

Cyclophosphamide

78
Q

What are examples of intercalating agents?

A

Cisplatin, carboplatin

79
Q

What are examples of anti-tumour antibiotics?

A

Bleomycin, doxorubicin

80
Q

What are examples of drugs directed against spindle microtubules, inhibiting mitosis?

A

Vincristine

81
Q

What is the mechanism of action of antimetabolites?

A

Interfere with DNA and RNA synthesis

82
Q

What is the mechanism of action of alkylating agents?

A

Form covalent bonds in DNA

83
Q

What is the mechanism of action of intercalating agents?

A

Bind to DNA and so inhibit replication

84
Q

What is the mechanism of action of anti-tumour antibiotics?

A

Lead to inhibition of DNA synthesis

85
Q

What are the side effects of chemo?

A
  1. Bone marrow suppression - cellular nadir tends to occur at approx. 7-14 days
  2. N&V
  3. Mucositis - ulcers to mucous membranes, particularly oral, esp. with methotrexate
  4. Diarrhoea - usually transient
  5. Alopecia
  6. Tinnitus - associated with cisplatin
  7. Peripheral neuropathy
  8. Lethargy
  9. Anorexia
86
Q

What chemo regimes are used in ovarian cancer?

A

Carboplatin +/- paclitaxel

87
Q

What chemo regimes are used in endometrial cancer?

A

Reserved for metastatic disease
Carboplatin +/- paclitaxel
OR
Doxorubicin + cisplatin

88
Q

What chemo regimes are used in cervical cancer?

A

Cisplatin + radiotherapy

89
Q

What chemo regime is used in vulval cancer?

A

5-FU +/- cisplatin
(+RT if not fit for surgery)

90
Q

What is the most potent oestrogen in the reproductive years?

A

Estradiol, followed by estrone

91
Q

What is the most potent oestrogen in the menopause?

A

Estrone

92
Q

What are the two types of oestrogen receptor?

A

Alpha and beta

93
Q

Where are alpha oestrogen receptors found?

A

Endometrium
ovarian stroma cells
hypothalamus
bone
breast cancer cells

94
Q

Where are beta oestrogen receptors found?

A

Kidney; brain; bone; heart; lungs; intestinal mucosa; prostate; endothelial cells

95
Q

Which receptor is the chief mediator of oestrogen on bone?

A

Alpha

96
Q

How is oestrogen metabolised?

A

Primarily in the liver, by conjugation and hydroxylation
Conjugation = sulphate (primarily)
Hydroxylation = catalysed by cytochrome P450

97
Q

What will suppress hepatic SHBG production?

A

Androgens
Insulin
Corticoids
Progestogens
GH

98
Q

What type of drug is clomifene?

A

Selective oestrogen receptor modulator

99
Q

What is an alternative to NSAIDs/progesterone’s/COCP/anti-fibrinolytic in reducing menstrual blood loss?

A

Danazol - isoxazole derivative of ethinyl testosterone - however androgen-like effects tend to be unacceptable to pts.

100
Q

What is tibolone?

A

A synthetic steroid
estrogenic, progestogenic and androgenic properties
an alternative to combined continuous HRT

101
Q

What is meant by bioavailability?

A

The proportion of drug that reaches the circulation unchanged - IV drugs therefore have 100% bioavailability

102
Q

What is meant by volume of distribution?

A

Amount of drug in the whole body compared with its concentration in plasma.
Large Vd = drug sequestered in tissues

Theoretical volume of water in which the amount of drug would need to be uniformly distributed to produce an observed blood concentration

103
Q

What molecular weight must a drug be in order to be excreted by bile (and into faeces)?

A

> /= 300 Da

104
Q

What are the effects of enzyme inducers?

A

Result in increased activity of cytochrome p450 enzyme, and therefore lower levels of the drug

105
Q

What are some examples of enzyme inducers?

A

‘CRAPS’

Carbemazepine
Rifampicin
A - bArbiturates
Phenytoin
St John’s Wort

106
Q

What are the effects of enzyme inhibitors?

A

Inhibit hepatic metabolisms resulting in increased plasma levels of the drug, increasing the risk of toxicity and side effects

107
Q

What are some examples of enzyme inhibitors?

A

‘Some Certain Silly Compounds Annoyingly Inhibit Enzymes, Grrrr’
Sodium valproate
Cimetidine
Sulphonamides
Ciprofloxacin
Antifungals/amiodarone
Isoniazid
Erythromycin/clary
Grapefruit juice

108
Q

Which drugs do not cross the placenta?

A

HIT

Heparin (LMWH/unfractionated)
Insulin
Tubocarine (anaesthetic agent)

109
Q

When would a drug insult occur to cause limb reduction defects?

A

12-40 days

110
Q

When would a drug insult occur to cause anencephaly?

A

24 days

111
Q

When would a drug insult occur to cause transposition of the great vessels?

A

34 days

112
Q

When would a drug insult occur to cause cleft lip?

A

36 days

113
Q

When would a drug insult occur to cause VSD, syndactyly?

A

42 days

114
Q

When would a drug insult occur to cause hypospadias?

A

84 days

115
Q

Which drugs are teratogenic?

A

‘All the A’s’
1. AEDs
2, Abx
3. Anticoagulants
4. Antimetabolites
5. Antipsychotics
6. Acne drugs
7. Androgens
8. Alcohol

116
Q

Which drugs are contraindicated in breastfeeding?

A

Abx: tetracycline, metronidazole, chloramphenicol
Aspirin
Amiodarone
Cytotoxics
COCP
Lithium
Sedatives: benzo/barbiturates
Theophylline

117
Q

Which AED can cause hirsutism?

A

Phenytoin

118
Q

What is the mechanism of action of cabergoline?

A

Dopamine receptor D2 agonist

119
Q

What is phase 4 of the human drug trials?

A

Post-marketing surveillance

120
Q

What are the drugs that can cause abortion - using acronym MET?

A

M - misoprostol
E - ergotamine
T - thrombolytics

121
Q

When does neonatal narcotics abstinence syndrome usually present?

A

Within 48 hours of delivery

122
Q

Why may neonatal narcotics abstinence syndrome present beyond 48 hours after delivery?

A

It may occur up to 4/52 after delivery because methadone can be stored in the neonatal liver, lung and spleen

123
Q

What are the fetal affects of cocaine?

A
  1. FGR
  2. Fetal death
  3. Placental abruption
124
Q

What are the features of fetal alcohol syndrome?

A

Growth - LBW
Craniofacial abnormalities - flat philtrum
CNS abnormalities - microcephaly, agenesis of the corpus callosum, cerebellar hypoplasia
Neurodevelopmental - epilepsy, hearing loss, cognitive deficit

125
Q

What are the different groups of penicillins?

A
  1. Beta-lactams
  2. Beta-lactamase resistant
  3. Broad-spectrum penicillins
  4. Antipseudomonal penicillins
  5. Mecillinams
126
Q

What type of drug is oseltamivir?

A

Neuraminidase inhibitor

127
Q

What are the side effects of HAART?

A
  1. Lactic acidosis
  2. Hyperglycaemia
  3. Hepatitis
  4. Pancreatitis
  5. Peripheral neuropathy
128
Q

What is the HIV therapy regime used if a woman is not taking antiretrovirals at time of pregnancy?

A

START (short-term anti-retroviral therapy) - a HAART regime starting between weeks 20 and 28 and being discontinued shortly after delivery

129
Q

Which anti-malarial chemo-prophylaxis is safe to use in pregnancy?

A

Malarone
Mefloquine

130
Q

What would be the choices for malarial treatment in pregnancy in the UK?

A

Quinine (falciparum)
Chloroquine (non-falciparum)
Artesunate

131
Q

How is oxytocin excreted?

A

Bile
Urine

132
Q

What is the half-life of misoprostal?

A

40 mins

133
Q

What are the side effects of misoprostal?

A

Uterine hyperstimulation or rupture
Amniotic fluid embolism
D+V
Headache

134
Q

Which prostaglandin is used in PPH and termination of pregnancy?

A

Prostaglandin E1

135
Q

Which receptors do ergometrine work on?

A

5HT1
Dopamine
alpha-adrenergic

136
Q

What are the contraindications to atosiban?

A

Pre-eclampsia
Intrauterine death
Intrauterine infection
APH
Premature ROM after 30 weeks

137
Q

Is nifedipine licensed in pregnancy?

A

No

138
Q

What is the dual mechanism of action of methyldopa?

A
  1. Centrally acting alpha-2-agonist
  2. Competitive inhibitor of DOPA decarboxylase
139
Q

Aside from IUGR, what is a side effect of labetalol?

A

Neonatal hypoglycaemia

140
Q

What is the mechanism of action of labetalol?

A

Mixed alpha-1-beta blocker

141
Q

What is the effect of thiazide diuretics in pregnancy?

A

Neonatal thrombocytopneia

142
Q

What is the effect of statin in pregnancy?

A

CNS and limb defects

143
Q

How much does AED use increase the risk of teratogenicity in pregnancy?

A

x3

144
Q

What are the symptoms of neonatal BZD withdrawal syndrome?

A
  1. Hypotonia
  2. Reluctance to suckle
  3. Cyanosis
  4. Impaired metabolic response to cold stress
145
Q

Is warfarin embryopathy dose-dependant?

A

Yes

146
Q

What is the antidote to unfractionated heparin?

A

Protamine sulphate

147
Q

What can PPIs cause in pregnancy?

A

Anencepahly

148
Q

What can antacids in pregnancy cause?

A

Milk-alkali syndrome

149
Q

Where dose loperamide act?

A

Opioid receptors of the large bowel

150
Q

What is the affect of NSAIDs?

A

Inhibits prostaglandin synthesis by inhibiting COX1 and COX2

151
Q

What are the side effects of 5-ASAs used in pregnancy in mothers with UC/Crohn’s

A

Agranulocytosis
Hypospermia

152
Q

Why is PTU preferred over carbimazole in pregnancy?

A

Lower placental transfer and excretion in breast milk

153
Q

What are the uses of mifepristone?

A
  1. EC - delays ovulation and prevents implantation
  2. TOP (600mg) - up to 9/40
154
Q

What are the contraindications of mifepristone?

A
  1. Severe asthma
  2. Chronic renal failure
  3. Ectopic
  4. Acute porphyria
  5. Hepatic impairment
155
Q

What is the most effective form of contraception, and its pearl index?

A

Implanon at PI <0.1

156
Q

When can a COCP be used in breastfeeding vs. non-breastfeeding women?

A

Breastfeeding = >6 weeks post-partum ( but can reduce breast milk output)
Non-breastfeeding = >3 weeks post-partum

157
Q

What are the differences in dosing between high, standard and low strength oestrogen with regard to COCP?

A

Low = 20 micrograms
Standard = 30-35 grams
High = 50 micrograms

158
Q

Describe first generation COCPs:

A

High strength oestrogen 50 micrograms

159
Q

Describe second generation COCPs:

A

Standard strength oestrogen 30-35 micrograms

160
Q

Describe third generation COCPs:

A

Contain new-type progesterones

161
Q

What are the risks of new-type progesterones used in third generation COCPs?

A

Increased VTE risk

162
Q

What are the advantages of new-type progesterones used in third generation COCPs?

A

Reduced acne, weight gain, breast symptoms, headache and breakthrough bleeding

163
Q

What are the first and second generation progesterones?

A

Levonorgestrel
Norethisterone

164
Q

What are the third generation progesterones?

A

Desoegestrel
Gestodene

165
Q

What are the missed pill rules in COCP?

A

Missed 1 - take missed pill
Missed 2 - take missed pill + condoms

Missed 3+ take missed pill, condoms 7/7
- if in 3rd week, omit pill-free week,
- if in 1st week, use EC

Missing 3+ = 2 in low-strength oestrogen

166
Q

By how much is the risk of endometrial and ovarian cancer risk reduced by COCP?

A

Endometrial - 50% reduced risk, and remains reduced for >20 years after stopping COCP
Ovarian - 40-80% reduced risk in a >10 year user

167
Q

Which cancers do COCP increase the risk of?

A

Breast and cervical cancer

168
Q

What are the missed pill rules with POP?

A

Take missed or late pill (>3 hours with all POPs except cerazette when only late if >12hours delay), extra pre-caution for 48 hours

169
Q

What are the bleeding patterns seen in POP?

A

Amenorrhoea - 20%
Regular bleeding - 40%
Erratic bleeding - 40%

170
Q

When may women not breastfeeding have Depo-provera injection for contraception?

A

5 days post-partum

171
Q

What are the side effects of Depo?

A
  1. Weight gain - 2kg/year in 70%
  2. Osteoporosis - should not be used for >2 years
  3. Delay in return of fertility for 6-18 months
172
Q

When are peak progesterone levels after insertion of the implanon?

A

1-13 days

173
Q

When are ovulation-inhibiting levels of progesterone reached on insertion of the implanon?

A

Within 24 hours

174
Q

What proportion of women ovulate within 3 weeks of implanon removal?

A

90%

175
Q

When is the copper coil effective after insertion?

A

Effective immediately

176
Q

When is the Mirena coil effective after insertion?

A

If on day 1 cycle, immediately, otherwise, requires 7 days of precautions

177
Q

What are the complications of IUDs?

A
  1. 5% risk of expulsion, esp. in first 3/12
  2. Uterine perf - 1/1000
  3. Pelvic infection - risk greatest in first 20 days

P1EXAM (27 decks)

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