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Module 203 > 203 Drugs > Flashcards

203 Drugs Flashcards

1
Q

Fludrocortisol

A

Used for mineralocorticoid replacement therapy instead of aldosterone due to the short half-life of aldosterone

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2
Q

Glucocorticoids e.g. hydrocortisone

A

Used for:
Glucocorticoid replacement therapy;
Immunosuppressive or anti-inflammatory effects for arthritis, asthma, or allergies;
Treatment of proliferative conditions e.g. leukaemia

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3
Q

Hydrocortisone (cortisol)

A

Acts via specific intracellular glucocorticoid receptors to influence gene expression
Used as an anti-inflammatory agent and immunosuppressant
Drug of choice for hormone replacement therapy
Standard dose =15-20mg per day in divided doses
Adverse effects: hyperglycaemia, osteoporosis, Cushing’s syndrome
Oral bioavailability = 60-80%
High protein binding ability
Hepatic metabolism with a half life of 1.5

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4
Q

Propylthiouracil (PTU)

A

Drug of choice to treat hyperthyroidism in first trimester
Used to treat hyperthyroidism including Graves’ disease
Inhibits thyroperoxidase and inhibits tetraiodothyronine deiodinase (converts T4 to T3)
Standard dose = 50-150mg/day
Oral bioavailabilty = 80-95%
70% protein binding
90& hepatic glucuronidation
Half-life of 2hrs
Renal excretion
Adverse effects: rashes and pruritus are common (rx with antihistamines); agranulocytosis; serious liver injury, liver failure and death

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5
Q

Carbimazole

A 
Used to treat hyperthyroidism
Prodrug therefore converted to methimazole which prevents peroxidase iodinating tyrosine residues on thyroglobulin, hence reducing the production of the thyroid hormones (T3 & T4)
Standard dose: 5-15mg/day
More than 90% oral bioavailability
85% protein bound
Rapidly metabolised to methimazole
Half-life of 6.4hrs
90% excreted in urine as metabolites
Adverse effects: rashes and pruritus are common, neutropenia, agranulocytosis, teratogenic
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6
Q

Levothyroxine sodium

A

Used to treat thyroid deficiency (myxoedema, diffuse non-toxic goitre, hashimoto’s thyroiditis/lymphadenoid goitre, thryoid carcinoma)
Used to suppress TSH secretion in treatment of thyroid tumours
Given orally or by injection
Standard maintenance dose = 50-100 micrograms/day
100% bioavailability
More than 99% protein bound
Metabolised in liver by glucuronidation
Half-life of approx. 7days
20-40% excreted in urine
Adverse effects: at excessive doses palpitations, arrhythmias, diarrhoea, insomnia, tremor, weight loss, diarrhoea, vomiting, anginal pain, tachycardia

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7
Q

What drugs are associated with hyperprolactinaemia?

A

Antidepressants and antipsychotics (antidopaminergic action e.g. risperidone, trazodone, duloxetine)
Drugs for nausea and vertigo e.g. phenothiazines, metoclopramide, domperidone

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8
Q

Dopaminergic drugs

A

Cabergoline

Bromocriptine

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9
Q

Use of dopaminergic drugs

A

Treatment for prolactinoma, increases dopaminergic inhibition of prolactin to reduce prolactin production and shrink adenoma

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10
Q

Mechanism of action of Insulin

A

Affects all major metabolic pathways in liver, adipose tissue, and skeletal muscle
Net effect is to cause hypoglycemia and increase fuel storage in muscle, fat tissue and liver

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11
Q

Effect of Insulin on hepatocytes

A

decreases gluconeogenesis, glycogenolysis, ketogenesis, (increases glycogen synthesis)

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12
Q

Effect of insulin on muscle cells

A

increases GLUT-4 translocation to the membrane and hence increase glucose uptake, glucose oxidation, glycogen synthesis, amino acid uptake, protein synthesis
decreases glycogenolysis, amino acid release

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13
Q

Effect of insulin on adipocytes

A

increase glucose uptake, increase triglyceride synthesis; decrease FFA and glycerol release

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14
Q

Examples of sulfonylureas

A

Gliclazide
Glipizide
Glimepiride

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15
Q

Primary mechanism of action of sulfonylureas

A

Stimulates endogenous insulin release
Blocks ATP-sensitive K+ channel so potassium accumulates to depolarise beta cells. VGCCs open to allow calcium ions in and this mobilises vesicles to release endogenous insulin into the circulation

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16
Q

Secondary mechanism of action of sulphonylureas

A

Sensitise beta cells to glucose
Decrease lipolysis
Decrease clearance of insulin by the liver

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17
Q

Therapeutic uses of sulfonylureas

A

Useful in T2DM only - over 40yo, DM duration less than 10yrs, daily insulin (if taking) less than 40 units
Used in combo with other anti-diabetic drugs

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18
Q

Side effects of sulfonylureas

A

Hypoglycaemia

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19
Q

Side effects of Biguanides

A 
Lactic acidosis
Nausea
Vomiting
Anorexia
VitB12/folate deficiency (chronic use)
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20
Q

Example of biguanides

A

Metformin

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21
Q

Mechanism of action of biguanides

A

Increase glucose uptake in muscle
Decrease glucose production by liver through AMPK which increases expression of nuclear transcription factor SHP and this inhibits the expression of hepatic gluconeogenic genes PEPCK and glucose-6-phosphatase

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22
Q

Properties of metformin

A

Orally active
Excreted unchanged in urine - half-life 1.3-4.5hrs
Often combined in a single pill

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23
Q

Carbergoline

A

Dopamine agonist

used to normalise IGF-1

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24
Q

What is used to normalise IGF-1 in acromegaly?

A

Carbergoline
Long-acting somatostatin analogue
Pegvisomant (GH receptor antagonist)

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25
Q

Pegvisomant

A

GH receptor antagonist

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26
Q

Long-acting somatostatin analogue

A

Octreotide

Used for long and short term treatment of acromegaly

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27
Q

Tamoxifen

A

Anti-oestrogen inducing gonadotrophin release by occupying oestrogen receptors in the hypothalamus to interfere with feedback mechanism
Used for treating gynaecomastia and breast cancer
Works as an antagonist at ER-alpha
Works as an agonist at ER-beta

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28
Q

Testosterone therapy

A

Gel, injection, buccal, patch, or pellet
Used for hypogonadism
Main problem = infertility

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29
Q

Fertility treatment options

A 
Oestrogen antagonist
LH and FSH
FSH only 
Chorionic gonadotrophin
Progesterone/progestogens
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30
Q

Oestrogen antagonist for fertility

A

Suppresses negative feedback of oestrogen on the anterior pituitary gland to increase LH and FSH production
Allows follicular development
Given for a few days to free the system of negative feedback and increase LH and FSH

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31
Q

LH and FSH for fertility

A

Injected or nasal spray
Limited number of days of FSH given before a large dose of LH to induce ovulation
Induces fertility by mimicking the natural menstrual cycle

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32
Q

Progesterone/progestogens for fertility

A

Used for luteal insufficiency as not enough progesterone is secreted to get a healthy state therefore administered during the second half of the cycle

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33
Q

Female Oral Contraceptives

A

COCP

Progesterone only pill

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34
Q

COCP

A

Oestrogen and progesterone

Prevents follicular development and progestogens thicken mucus, prevent ovulation and create a hostile endometrium

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35
Q

Progesterone only pill

A

Thicken mucus, prevent ovulation and create a hostile endometrium
Inhibits LH surge hence no ovulation

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36
Q

Examples of POP

A

Norethisterone
Levonorgestrel
Desogestrel

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37
Q

Adverse effects of POP

A

Nausea, menstrual irregularity, vomiting, headache, breast discomfort, weight changes, changes in libido

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38
Q

Properties of POP

A 
Administered once a day 
65-80% oral bioavailability
High protein binding
Hepatic metabolism
Half-life of 10hrs
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39
Q

COCP

A

Progestogen and oestrogen e.g. norethisterone and ethinyloestradiol
Progestogen inhibits ovulation by suppression of LH surge, thickens cervical mucus, renders endometrium hostile
Oestrogen prevents follicular development by suppression of FSH

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40
Q

Why POP over COCP?

A

Woman has had oestrogen dependent tumours, overweight woman who smokes (don’t want to further increase DVT risk), DVTs, cervical problems, etc.

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41
Q

Properties of COCP

A

1 tablet per day for 21days then 7days off
20-35g ethinyloestradiol
500-1000mcg norethisterone

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42
Q

IUS

A

Mirena or Jaydess
Releases progestogen
3-5yrs use

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43
Q

IUD

A

Copper coil on T-shaped plastic - spermicide

5-10yrs use

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44
Q

Implants

A

Last for 3-5yrs

Subcutaneous insertion and removal by professional

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45
Q

Vaginal ring

A

Inserted into vagina and releases progestogens
Must be inserted by individual and left for 21days then removed for 7day withdrawal bleed
Must be removed for coitus but must be inserted within 3hrs of removal

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46
Q

Other uses for contraceptives

A

Dysmenorrhoea (painful periods)

Heavy menstrual bleeding

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47
Q

Levonorgestrel

A

Emergency contraceptive

Blocks ovulation if it hasn’t occurred already otherwise ineffective

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48
Q

Ulipristal

A

Emergency contraceptive
Progesterone partial agonist
Blocks progesterone receptors to stop the endometrium developing

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49
Q

Mifepristone

A 
Competitive Progesterone receptor antagonist used for abortions
Endometrium collapses (degeneration) and softening/dilatation of cervix - can be used for up to 3months of pregnancy
50
Q

Male contraceptives

A

Testosterone - blocks LH and FSH production from anterior pituitary glands by stimulating negative feedback
Not trusted by women

51
Q

In what ways can drugs act?

A

Agonist (mimic natural hormone/transmitter)
Antagonist (block effects of a natural hormone/transmitter)
Induce synthesis of a natural hormone/transmitter
Block synthesis of a natural hormone/transmitter
Induce metabolism of a natural hormone/transmitter
Block metabolism of a natural hormone/transmitter

52
Q

Effects of GH

A

Promote linear growth of adolescence by increasing protein synthesis and collagen deposition

53
Q

Uses of GH

A

GH deficiency in children and adults
Prader-Willi syndrome, Turner’s syndrome, chronic renal insufficiency in children
Licensed for use in short children considered small for gestational age at birth

54
Q

Somatropin

A

synthetic GH

55
Q

Cautions with somatropin

A

DM, papilloedema, relative deficiencies in pituitary hormones (hypothyroidism), disorders of epiphysis of the hip, history of malignant disease

56
Q

Contraindications with somatropin

A

Tumour activity evidence, renal transplantation, severe obesity or respiratory impairment in Prader-Willi syndrome, pregnancy

57
Q

Side effects with somatropin

A

Headache, papilloedema, fluid retention, arthralgia, myalgia, carpel tunnel syndrome, insulin resistance, hyperglycaemia, hypoglycaemia, leukaemia

58
Q

Somatomedins

A

Polypeptide hormones related to insulin (aka IGFs)

59
Q

Mecasermin

A

human IGF-1 used to treat growth failure in children and adolescents with severe primary in Insulin-like growth factor-1 deficiency

60
Q

Cautions for Mecasermin

A 
Hypothyroidism
DM
Monitor ECG before nad after treatment initiation
Papilloedema
Disorders of epiphysis of hip
Pregnancy
61
Q

Contraindications for Mecasermin

A

Tumour activity evidence

Breastfeeding

62
Q

Side effects for Mecasermin

A 
Headache
Tachycardia
Cardiomegaly
Hyperglycaemia
Ventricular hypertrophy
Convulsions
Sleep apnoea
Night terrors
Dizziness
Gynaecomastia
Arthralgia
Myalgia
63
Q

Pegvisomant

A

Genetically modified analogue of human growth hormone

Selective GH antagonist

64
Q

Uses of pegvisomant

A

Acromegaly in patients with inadequate response to surgery or radiation
Only used by physicians experienced in acromegaly treatment

65
Q

Cautions for pegvisomant

A

Liver disease (monitor liver enzymes every 4-6 weeks for 6months)
DM
Possible increase in female fertility

66
Q

Contraindications for pegvisomant

A

Pregnancy

Breastfeeding

67
Q

Side effects of pegvisomant

A 
Diarrhoea
Constipation
Nausea
Vomiting
Abdominal distension
Dyspepsia
Flatulence
Elevated liver enzymes
Hypertension
Headache
Hypergylcaemia
Hypoglycaemia
Influenza-like syndrome
May see thrombocytopenia, leucopenia, leucocytosis, bleeding tendency
68
Q

Liothyronine sodium

A

Similar to levothyroxine but more rapidly metabolised and has more rapid effect
Effects develop after a few hrs and disappear after 24-48hrs of Rx discontinuation
Used for severe hypothyroid states e.g. hypothyroid coma (IV use)

69
Q

Cautions of levothyroxine sodium

A 
Panhypopituitarism or predisposition to adrenal insufficiency
Elderly
CV disorders
DM
DI
Pregnancy
70
Q

Thyrotropin alfa

A

Recombinant form of thyrotropin (TSH)
Used with/out radioiodine imaging with serum thyroglobulin testing to detect thyroid remnants and thyroid cancer in post-thyroidectomy pts

71
Q

Antithyroid drugs

A

Used for hyperthyroidism to prepare pt for thyroidectomy or long-term Rx
E.g. Carbimazole, Propylthiouracil

72
Q

Propylthiouracil

A

Used in pts who suffer sensitivity reactions to carbimazole

Interferes synthesis of thyroid hormones

73
Q

Natural oestrogens

A

Oestradiol
Oestrone
Oestriol
More appropriate for HRT than synthetic oestrogens
Not used to suppress lactation because of association with thromboembolism

74
Q

Tibolone

A

Oestrogenic, progestogenic, and weak androgenic activity
Used for short-term Rx of oestrogen deficiency and for osteoporosis prophylaxis
Cautions: vaginal bleeding, renal impairment, history of liver disease, epilepsy, migraine, DM, hypercholesteraemia
Contraindications of tibolone: hormone-dependent tumours, history of cardiovascular or cerebrovascular disease, severe liver disease, pregnancy, breastfeeding
Side effects: abdo pain, weight changes, vaginal bleeding, facial hair, GI disturbances, oedema, dizziness, headache, migraine, depression, breast cancerAdverse effects
Nausea, vomiting, abdominal cramps, fluid retention, changes in body weight, hepatic impairment. Cardiovascular changes including DVT, breast tenderness, cervical erosion. Exacerbation of migraine. Chloasma.

75
Q

HRT

A

Small oestrogen dose (with progestogen in women with uterus)

Used in women with natural or surgical menopause before 45 due to increased risk of osteoporosis

76
Q

Topical vaginal oestrogen

A

Used for short-course Rx of menopausal atrophic vaginitis

77
Q

Adverse effects of COCP

A

Nausea, vomiting, abdominal cramps, fluid retention, changes in body weight, hepatic impairment. Cardiovascular changes including DVT, breast tenderness, cervical erosion. Exacerbation of migraine. Chloasma.

78
Q

Selective Oestrogen Receptor Modulator (SERM)

A

Binds to oestrogen receptors of bone to prevent osteoporosis

79
Q

Raloxifene hydrochloride

A

Selective oestrogen receptor modulator (SERM)
Acts at ER-beta which are located in bone
Indicated for Rx and prevention of postmenopausal osteoporosis, can be used for vasomotor symptoms in menopause
Cautions: risk factors for VTE, breast cancer, history of oestrogen-induced hypertriglyceridaemia
Contraindications: history of VTE, undiagnosed uterine bleeding, endometrial cancer, hepatic impairment, pregnancy, breastfeeding, severe renal impairment
Side effects: VTE, thrombophlebitis, hot flushes, leg cramps, peripheral oedema, influenza-like symptoms

80
Q

Anti-oestrogens

A

E.g. clomifene and tamoxifen used in treatment of female infertility due to oligomenorrhoea or secondary amenorrhoea e.g. associated with polycystic ovarian disease
Induce gonadotrophin release by occupying oestrogen receptors in the hypothalamus interfering with feedback mechanism
Risk of multiple pregnancy

81
Q

Tamoxifen

A

Effective in premenopausal, perimenopausal, postmenopausal women

82
Q

Aromatase inhibitors

A

Anastrozole
Exemestane
Letrozole
Effective for breast cancer treatment in postmenopausal women

83
Q

Infertility treatment with proven hypopituitarism, not responding to clomifene, superovulation treatment for assisted conception

A

LH and FSH
FSH only
Chorionic gonadotrophin

84
Q

Unusual uses of gonadotrophins

A

Hypogonadotrophic hypogonadism and associated oligospermia

85
Q

Treatment for delayed puberty in male

A

Chorionic gonadotrophin to stimulate endogenous testosterone production
Testosterone

86
Q

Caution for human menopausal gonadotrophins

A

Rule out infertility caused by hypothyroidism, adrenocortical deficiency, hyperprolactinaemia, tumours of pituitary or hypothalamus

87
Q

Contraindications for human menopausal gonadotrophina

A 
Ovarian cysts
Tumours of pituitary, hypothalamus, breast, uterus, ovaries, testes or prostate
Vaginal bleeding of unknown cause
Pregnancy
Breastfeeding
88
Q

Side effects of human menopausal gonadotrophins

A 
Ovarian hyperstimulation
Increased risk of multiple pregnancy and miscarriage
Hypersensitivity reactions
GI disturbances
Headache
Joint pain
Fever
Injection site reactions
Rare: thromboembolism, gynaecomastia, acne, weight gain
89
Q

Gonadorelin

A

IV injection to increase plasma concentrations of LH and FSH

Not useful in distinguishing hypothalamic from pituitary lesions

90
Q

Gonadorelin analogues

A

Use in endometriosis, infertility, breast cancer, prostate cancer, precocious puberty, anaemia due to uterine fibroids, before intrauterine surgery

91
Q

Leuprorelin and triptorelin

A

Taken for 3-4months
Reduces uterine volume, fibroid size and associated bleeding
Makes vaginal procedures more feasible for women undergoing hysterectomy or myomectomy

92
Q

Bisphosphonates

A

For osteoporosis prevention in menopausal women

E.g. alendronate, risedronate

93
Q

Contraindications of HRT

A

pregnancy, active VTE, severe acute liver disease, endometrial cancer with recurrence, breast carcinoma with recurrence

94
Q

Cautions with HRT

A

Abnormal bleeding, breast lump, previous endometrial cancer/breast cancer, strong family history of breast cancer, family history of thromboembolism

95
Q

Misoprostol

A

Synthetic prostaglandin analogue
Used for abortions/termination after mifepristone
Stimulates uterine contractions and effacement of the cervix

96
Q

Aldosterone antagonist

A

E.g. spironolactone, eplerinone
Used for primary hyperaldosteronism/Conn’s syndrome due to unilateral adenoma or bilateral hyperplasia
Spironolactone may disrupt oestrogen to cause gynaecomastia in males, and disrupt menstrual cycles in women

97
Q

Alpha blockers and beta blockers

A

Alpha blockers e.g. phenoxybenzamine, doxazocin
Beta blockers e.g. propanolol
Used for hypertension associated with phaeochromocytoma

98
Q

Orlistat

A

Used for weight loss in obese or overweight patients
Binds and inhibits lipases in the lumen of the gut to prevent hydrolysis of dietary fat into absorbable free fatty acids
Results in 1/3 of dietary fat passing out in stool (steatorrhoea)
Side effects: flatulence, oily faecal leakage, diarrhoea

99
Q

Metformin

A

Oral hypoglycaemia agent used for T2DM management in obese/overweight patients

100
Q

Routes of administration of insulin

A

Intravenous
Intramuscular
Subcutaneous

101
Q

Thiazolidinediones

A

Glitazones e.g. pioglitazone
Decreases insulin resistance by activating PPAR-gamma which increases transcription of genes that increase insulin response and regulate adipocyte lipid metabolism

102
Q

Side effects of thiazolidinediones

A

Fluid retention
Weight gain
Possible liver failure
May lower effectiveness of COCP

103
Q

GLP-1 analogues

A

Increases glucose-dependent insulin secretion
Decreased appetite, increased satiety
Decreased pancreatic release of glucagon
Decreased gastric emptying
Side effect: GI disturbances e.g. heartburn, diarrhoea, belching

104
Q

DPP-4 inhibitors

A

Vildagliptin or Sitagliptin
Increases GLP-1 to increase glucose-dependent insulin secretion, decrease hepatic glucagon secretion, decrease appetite and decrease gastric emptying

105
Q

Side effects of DDP-4 inhibitors

A

Possible risk of cancer as DDP-4 acts as a tumour suppressor

106
Q

SGLT-2 inhibitors

A

Dapagliflozin
Inhibits renal tubular sodium-glucose co-transporter to reverse hyperglycaemia, increase beta cell function, increase GLUT4 translocation, increase insulin signalling

107
Q

Side effects of SGLT-2 inhibitors

A

Glycosuria causes increased weight loss and increased risk of UTIs

108
Q

Anti-androgens

A

GIVEN WITH COCP
Cyproterone acetate - prevents testosterone and DHT binding to androgen receptors
Spironolactone - weak anti-androgenic effects

109
Q

Eflornithine cream

A

Inhibits ornithine decarboxylase in hair follicles

Used for hirsuitism

110
Q

Glucocorticoid and Mineralocorticoid replacement therapy

A

Used for congenital adrenal hyperplasia seen in children

111
Q

Treatment of CAH in adults

A

Presentation is mild resembling PCOS therefore treated like PCOS with COCP with/out anti-androgen

112
Q

Letrozole

A

Aromatase inhibitor
Inhibits testosterone conversion to oestrogen
Used to treat steroid hormone receptor positive breast cancer

113
Q

Cinacelet

A

Calcium receptor agonist

Used for tertiary hyperparathyroidism

114
Q

SSRIs for men

A

Can be used for premature orgasm or ejaculation

Side effects include erectile dysfunction

115
Q

Therapeutic options for erectile dysfunction

A

PDE5 inhibitor: Viagra, Levitra, Spedra, Cialis (tadalafil)
Never prescribe with GTN as can lead to catastrophic CV collapse
Topical or injection of prostaglandins
Testosterone gel
Vacuum device
Penile implant

116
Q

Cialis

A

Le Weekend/Tadalafil
Taken at least 30 minutes before sexual activity (starts working within 6mins)
Half-life of 17.5hrs

117
Q

Side effects of synthetic prostaglandin E1

A

Priapism (need to drain penis)
Pain
Fibrosis

118
Q

Medications reducing sexual desire

A 
Antidepressants
Antipsychotics
Antihypertensives
Anti-cancer drugs
Oral contraceptives
119
Q

Botox

A

Administered to pelvic floor muscles for vaginismus to relieve dyspareunia

120
Q

Oestrogen creams

A

Improve local pelvic floor and skin

Do not increase breast cancer risk

121
Q

Dexamethasone/Betamethasone

A

Used to assist maturation of lungs in premature babies as it stimulates the alveoli cells to produce surfactant genes
Prevents neonatal respiratory distress syndrome

122
Q

Rx for PPH

A

Ergotamine (vasoconstrictor) or tranexamic acid - to stop blood loss
IV fluids

Module 203 (10 decks)

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