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Module 203 > 203 Drugs > Flashcards

203 Drugs Flashcards

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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
Pegvisomant
GH receptor antagonist
26
Long-acting somatostatin analogue
Octreotide | Used for long and short term treatment of acromegaly
27
Tamoxifen
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
28
Testosterone therapy
Gel, injection, buccal, patch, or pellet Used for hypogonadism Main problem = infertility
29
Fertility treatment options
``` Oestrogen antagonist LH and FSH FSH only Chorionic gonadotrophin Progesterone/progestogens ```
30
Oestrogen antagonist for fertility
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
31
LH and FSH for fertility
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
32
Progesterone/progestogens for fertility
Used for luteal insufficiency as not enough progesterone is secreted to get a healthy state therefore administered during the second half of the cycle
33
Female Oral Contraceptives
COCP | Progesterone only pill
34
COCP
Oestrogen and progesterone | Prevents follicular development and progestogens thicken mucus, prevent ovulation and create a hostile endometrium
35
Progesterone only pill
Thicken mucus, prevent ovulation and create a hostile endometrium Inhibits LH surge hence no ovulation
36
Examples of POP
Norethisterone Levonorgestrel Desogestrel
37
Adverse effects of POP
Nausea, menstrual irregularity, vomiting, headache, breast discomfort, weight changes, changes in libido
38
Properties of POP
``` Administered once a day 65-80% oral bioavailability High protein binding Hepatic metabolism Half-life of 10hrs ```
39
COCP
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
40
Why POP over COCP?
Woman has had oestrogen dependent tumours, overweight woman who smokes (don't want to further increase DVT risk), DVTs, cervical problems, etc.
41
Properties of COCP
1 tablet per day for 21days then 7days off 20-35g ethinyloestradiol 500-1000mcg norethisterone
42
IUS
Mirena or Jaydess Releases progestogen 3-5yrs use
43
IUD
Copper coil on T-shaped plastic - spermicide | 5-10yrs use
44
Implants
Last for 3-5yrs | Subcutaneous insertion and removal by professional
45
Vaginal ring
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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Other uses for contraceptives
Dysmenorrhoea (painful periods) | Heavy menstrual bleeding
47
Levonorgestrel
Emergency contraceptive | Blocks ovulation if it hasn't occurred already otherwise ineffective
48
Ulipristal
Emergency contraceptive Progesterone partial agonist Blocks progesterone receptors to stop the endometrium developing
49
Mifepristone
``` 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
Male contraceptives
Testosterone - blocks LH and FSH production from anterior pituitary glands by stimulating negative feedback Not trusted by women
51
In what ways can drugs act?
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
Effects of GH
Promote linear growth of adolescence by increasing protein synthesis and collagen deposition
53
Uses of GH
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
Somatropin
synthetic GH
55
Cautions with somatropin
DM, papilloedema, relative deficiencies in pituitary hormones (hypothyroidism), disorders of epiphysis of the hip, history of malignant disease
56
Contraindications with somatropin
Tumour activity evidence, renal transplantation, severe obesity or respiratory impairment in Prader-Willi syndrome, pregnancy
57
Side effects with somatropin
Headache, papilloedema, fluid retention, arthralgia, myalgia, carpel tunnel syndrome, insulin resistance, hyperglycaemia, hypoglycaemia, leukaemia
58
Somatomedins
Polypeptide hormones related to insulin (aka IGFs)
59
Mecasermin
human IGF-1 used to treat growth failure in children and adolescents with severe primary in Insulin-like growth factor-1 deficiency
60
Cautions for Mecasermin
``` Hypothyroidism DM Monitor ECG before nad after treatment initiation Papilloedema Disorders of epiphysis of hip Pregnancy ```
61
Contraindications for Mecasermin
Tumour activity evidence | Breastfeeding
62
Side effects for Mecasermin
``` Headache Tachycardia Cardiomegaly Hyperglycaemia Ventricular hypertrophy Convulsions Sleep apnoea Night terrors Dizziness Gynaecomastia Arthralgia Myalgia ```
63
Pegvisomant
Genetically modified analogue of human growth hormone | Selective GH antagonist
64
Uses of pegvisomant
Acromegaly in patients with inadequate response to surgery or radiation Only used by physicians experienced in acromegaly treatment
65
Cautions for pegvisomant
Liver disease (monitor liver enzymes every 4-6 weeks for 6months) DM Possible increase in female fertility
66
Contraindications for pegvisomant
Pregnancy | Breastfeeding
67
Side effects of pegvisomant
``` 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
Liothyronine sodium
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
Cautions of levothyroxine sodium
``` Panhypopituitarism or predisposition to adrenal insufficiency Elderly CV disorders DM DI Pregnancy ```
70
Thyrotropin alfa
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
Antithyroid drugs
Used for hyperthyroidism to prepare pt for thyroidectomy or long-term Rx E.g. Carbimazole, Propylthiouracil
72
Propylthiouracil
Used in pts who suffer sensitivity reactions to carbimazole | Interferes synthesis of thyroid hormones
73
Natural oestrogens
Oestradiol Oestrone Oestriol More appropriate for HRT than synthetic oestrogens Not used to suppress lactation because of association with thromboembolism
74
Tibolone
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
HRT
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
Topical vaginal oestrogen
Used for short-course Rx of menopausal atrophic vaginitis
77
Adverse effects of COCP
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
Selective Oestrogen Receptor Modulator (SERM)
Binds to oestrogen receptors of bone to prevent osteoporosis
79
Raloxifene hydrochloride
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
Anti-oestrogens
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
Tamoxifen
Effective in premenopausal, perimenopausal, postmenopausal women
82
Aromatase inhibitors
Anastrozole Exemestane Letrozole Effective for breast cancer treatment in postmenopausal women
83
Infertility treatment with proven hypopituitarism, not responding to clomifene, superovulation treatment for assisted conception
LH and FSH FSH only Chorionic gonadotrophin
84
Unusual uses of gonadotrophins
Hypogonadotrophic hypogonadism and associated oligospermia
85
Treatment for delayed puberty in male
Chorionic gonadotrophin to stimulate endogenous testosterone production Testosterone
86
Caution for human menopausal gonadotrophins
Rule out infertility caused by hypothyroidism, adrenocortical deficiency, hyperprolactinaemia, tumours of pituitary or hypothalamus
87
Contraindications for human menopausal gonadotrophina
``` Ovarian cysts Tumours of pituitary, hypothalamus, breast, uterus, ovaries, testes or prostate Vaginal bleeding of unknown cause Pregnancy Breastfeeding ```
88
Side effects of human menopausal gonadotrophins
``` 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
Gonadorelin
IV injection to increase plasma concentrations of LH and FSH | Not useful in distinguishing hypothalamic from pituitary lesions
90
Gonadorelin analogues
Use in endometriosis, infertility, breast cancer, prostate cancer, precocious puberty, anaemia due to uterine fibroids, before intrauterine surgery
91
Leuprorelin and triptorelin
Taken for 3-4months Reduces uterine volume, fibroid size and associated bleeding Makes vaginal procedures more feasible for women undergoing hysterectomy or myomectomy
92
Bisphosphonates
For osteoporosis prevention in menopausal women | E.g. alendronate, risedronate
93
Contraindications of HRT
pregnancy, active VTE, severe acute liver disease, endometrial cancer with recurrence, breast carcinoma with recurrence
94
Cautions with HRT
Abnormal bleeding, breast lump, previous endometrial cancer/breast cancer, strong family history of breast cancer, family history of thromboembolism
95
Misoprostol
Synthetic prostaglandin analogue Used for abortions/termination after mifepristone Stimulates uterine contractions and effacement of the cervix
96
Aldosterone antagonist
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
Alpha blockers and beta blockers
Alpha blockers e.g. phenoxybenzamine, doxazocin Beta blockers e.g. propanolol Used for hypertension associated with phaeochromocytoma
98
Orlistat
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
Metformin
Oral hypoglycaemia agent used for T2DM management in obese/overweight patients
100
Routes of administration of insulin
Intravenous Intramuscular Subcutaneous
101
Thiazolidinediones
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
Side effects of thiazolidinediones
Fluid retention Weight gain Possible liver failure May lower effectiveness of COCP
103
GLP-1 analogues
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
DPP-4 inhibitors
Vildagliptin or Sitagliptin Increases GLP-1 to increase glucose-dependent insulin secretion, decrease hepatic glucagon secretion, decrease appetite and decrease gastric emptying
105
Side effects of DDP-4 inhibitors
Possible risk of cancer as DDP-4 acts as a tumour suppressor
106
SGLT-2 inhibitors
Dapagliflozin Inhibits renal tubular sodium-glucose co-transporter to reverse hyperglycaemia, increase beta cell function, increase GLUT4 translocation, increase insulin signalling
107
Side effects of SGLT-2 inhibitors
Glycosuria causes increased weight loss and increased risk of UTIs
108
Anti-androgens
GIVEN WITH COCP Cyproterone acetate - prevents testosterone and DHT binding to androgen receptors Spironolactone - weak anti-androgenic effects
109
Eflornithine cream
Inhibits ornithine decarboxylase in hair follicles | Used for hirsuitism
110
Glucocorticoid and Mineralocorticoid replacement therapy
Used for congenital adrenal hyperplasia seen in children
111
Treatment of CAH in adults
Presentation is mild resembling PCOS therefore treated like PCOS with COCP with/out anti-androgen
112
Letrozole
Aromatase inhibitor Inhibits testosterone conversion to oestrogen Used to treat steroid hormone receptor positive breast cancer
113
Cinacelet
Calcium receptor agonist | Used for tertiary hyperparathyroidism
114
SSRIs for men
Can be used for premature orgasm or ejaculation | Side effects include erectile dysfunction
115
Therapeutic options for erectile dysfunction
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
Cialis
Le Weekend/Tadalafil Taken at least 30 minutes before sexual activity (starts working within 6mins) Half-life of 17.5hrs
117
Side effects of synthetic prostaglandin E1
Priapism (need to drain penis) Pain Fibrosis
118
Medications reducing sexual desire
``` Antidepressants Antipsychotics Antihypertensives Anti-cancer drugs Oral contraceptives ```
119
Botox
Administered to pelvic floor muscles for vaginismus to relieve dyspareunia
120
Oestrogen creams
Improve local pelvic floor and skin | Do not increase breast cancer risk
121
Dexamethasone/Betamethasone
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
Rx for PPH
Ergotamine (vasoconstrictor) or tranexamic acid - to stop blood loss IV fluids

Module 203 (10 decks)

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