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S6 > Pharmacology > Flashcards

Pharmacology Flashcards

1
Q

Types of estrogen

A

Estradiol is the most potent , produced by ovary , the principal estrogen in premenopausal women.

Estrone is a metabolite of estradiol has one-third the estrogenic potency of estradiol, the primary circulating estrogen after menopause, generated from conversion of androstenedione in peripheral tissues.

Estriol metabolite of estradiol, significantly less potent than estradiol, present in significant amounts during pregnancy, produced by placenta.

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2
Q

Naturally occurring estrogens

A

Conjugated equine estrogens (Premarin)-natural
equilin (obtained from urine of pregnant mares)undergo some firstpass metabolism, but it is not sufficient to lessen the effectiveness when taken orally,

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3
Q

Synthetic estrogen analogs such as

A

ethinylestradiol, mestranol and estradiol valerate, analogs have a prolonged action and a higher potency compared to those of natural estrogens.

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4
Q

Estrogen actions

A

Actions

Side effects

Development of female genital tract Mild anabolic Normal function of skin & bl.vess. Sodium and water retention Raise HDL, lower LDL Decrease Bone Resorption Increase blood coagulability may Improve mood, concentration, reduce Alzheimer’s Disease

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5
Q

Estrogens side effect

A

Irregular withdrawal vaginal bleeding Breast tenderness Nausea, vomiting Water retention Increase coagulability, thromboembolism Impaired glucose tolerance Endometrial hyperplasia & cancer Cholestasis & gallbladder disease

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6
Q

Progesterone/ progestogens actions

A

Secretory endometrium Anabolic Increase Bone Mineral Density Fluid retention Mood changes( depressant)

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7
Q

Side effects of progesterone

A

Weight gain Fluid retention Acne Hirsutism Nausea vomiting Depression, PMS lack of concentration

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8
Q

Progesterone derivatives

Oral

A

Medroxyprogesterone, Dyhdrogesterone

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9
Q

Testosterone derivatives

Oral

A

Norethisterone, Norethindrone , norgestrel, Norgestimate

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10
Q

Testosterone

Actions/Side effects

A

Male secondary sex characteristics Anabolic Acne Voice changes Aggression Metabolic adverse effects on lipids
Dec HDL
WHILE ESTROGEN INC HDL

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11
Q

Implants form of E

Vaginal

A

Etonorgestrel

estradiol cream for vaginal atrophy

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12
Q

Testosterone Implants
IM
Oral

A

Testosterone

Enenthate, Proprionate

Undecanoate, Mesterolone

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13
Q

منو اكثر شي يتأثر بال first pass metabolism ايستروجين لو بروجستيرون

A

Transport bound to SHBG and albumin ➢ Liver metabolism, progesterone almost metabolised in one passage through liver ➢ Metabolites excreted in Urine (as glucuronides and sulphates)

In estrogen no effect of fast effect metabolism
But in progesterone effect is higher

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14
Q

Combined Oral Contraceptive Pill

A

Oestrogens: high/low dose: 50, 35, 30, 20mg/day

ethinylestradiol mestranol

Progestogens: which generation?

1 st : norethynodrel 2 nd : levonorgestrel, norethisterone 3 rd : desogestrel, gestodene, norgestimate 4 th : drospirenone (Yasmin:antimineralocorticoid, antiandrogen), norelgestromin (Evra: patch)

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15
Q

Progestogens: which generation?

A

1 st : norethynodrel 2 nd : levonorgestrel, norethisterone 3 rd : desogestrel, gestodene, norgestimate 4 th : drospirenone (Yasmin:antimineralocorticoid, antiandrogen), norelgestromin (Evra: patch)

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16
Q

Adverse Effects of COC

A

▪Venous thromboembolism ▪Myocardial infarction ▪Hypertension ▪Decrease glucose tolerance ▪Increase risk of stroke in women with focal migraine ▪Headaches ▪Mood swings ▪Cholestatic jaundice ▪Increase incidence of gallstones ▪Precipitate porphyria

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17
Q

The Mini-pill

COC طريقة أخذ الدواء

A

28 days progestogen
COC

Monophasic = 21

Triphasic = 21

Every Day: ED = 21+7 placebo

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18
Q

Other progestogens

Implant

A

Medroxy Progesterone Acetate

▪Depot provera: MPA

Etonogestrel

▪ Female implants: Implanon ▪ Male implants ▪Vaginal ring

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19
Q

POP side effect

A

Side-effects of all POPs include possible irregular bleeding, persistent ovarian follicles (simple cysts) and acne. If a POP is missed then the woman should continue taking the POP and use extra precautions (e.g. condoms) for the next 48 hours until the progestogen effect on the mucus is built up. If unprotected sex occurs during this time, then emergency contraception is required.

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20
Q

Steroids in HRT

A

Oestradiol e.g. valerate, enanthates, Micronised oestradiol,
 1-2mg/day
 Premarin 0.625-1.25mg/day

Medroxyprogesterone acetate (Provera) Norethisterone Duphaston

دوفاستون والمسمى بالدوديجسترول

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21
Q

Risks of HRT

A

▪Unopposed oestrogen: increase endometrial cancer, and ovarian cancer ▪Increased Breast cancer ▪Increased Ischaemic Heart Disease, and stroke ▪Increase risk of venous thromboembolism ▪Uterine bleeding

▪Adverse effect on lipid profile

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22
Q

SERM

A

Selective Estrogen Receptor Modulators

estrogen related compounds, which interact at estrogen receptors but have different effects on different tissues, so they display selective agonism or antagonism according to the tissue type

Raloxifene

Protects against osteoporosis ▪ No proliferative effects on endometrium ▪ No proliferative affect breast ▪ Increases hot flushes ▪increased risk of DVT, pulmonary embolism, & retinal vein thrombosis

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23
Q

Weak oestrogens that block receptors

A

Clomiphene: ovulation induction: inhibit oestrogen binding to anterior pituitary, inhibit negative feedback, results in increased GnRH and FSH, LH .Side effects : hot flushes, ovarian enlargement & risk of multiple pregnancy .

24
Q

Tamoxifen

A

used for treatment of metastatic breast cancer, or as adjuvant therapy following mastectomy or radiation for breast cancer , and as prophylactic therapy to reduce the risk of breast cancer in high-risk patients.

25
Q

Ospemifene

A

is indicated for the treatment of dyspareunia (painful sexual intercourse)

related to menopause.

26
Q

Mifepristone

A

progesterone antagonist inhibits progesterone action ▪ Sensitises the uterus to prostaglandins ▪ Used for medical termination of pregnancy with misoprostol, and induction of labour

27
Q

Anti-androgen

A

Cyproterone: Progesterone derivative

▪Weak progestogenic effect. Partial agonist to progesterone receptor, competes with dihydrotestosterone ▪Used in combined contraceptive pill (Dianette)
Finasteride
Flutamide

28
Q

inhibit 5α-reductase

Antiandrogen

A

Finasteride inhibit 5α-reductase resulting in decreased formation of dihydrotestosterone. used for the treatment of benign prostatic hyperplasia .

29
Q

competitive inhibitor of androgens

A

Flutamide act as competitive inhibitor of androgens at the target cell and are effective orally for the treatment of prostate cancer .

30
Q

Glucocorticoid (GC) action

A

Increased glucose production

  • Breakdown of protein
  • Redistribution of fat
  • Anti-inflammatory
  • Immunosuppression
31
Q

Corticosteroids and immune system

A

Inhibition of B and T cell responses

  • Reduced transcription of cytokines
  • Reduced cell adhesion by leucocytes
  • Reduced phagocytic function
  • Immune suppression
32
Q

Corticosteroid Replacement

A

Hydrocortisone

33
Q

Inflammatory

Disease

A

Prednisolone

34
Q

Tumour

Oedema

A

Dexamethasone

35
Q

Topical

Treatment

A

Betamethasone

36
Q

Mineralocorticoid

Replacement

A

Fludrocortisone

37
Q

Routes of administration

Intravenous

A

methylprednisolone

38
Q

Routes of administration

Oral

A

prednisolone

dexamethasone

hydrocortisone

fludrocortisone

39
Q

Routes of administration

Inhaled

A

fluticasone (high 1 stpass metabolism)

beclomethasone

40
Q

Routes of administration

Topical

A

flexor>forehead>scalp>face>forearm

betamethasone

41
Q

Routes of administration

Intra-articular

A

triamcinolone

depomedrone

42
Q

Summary of clinical use

A

Adrenal insufficiency

  • Inflammatory disease
  • Immuno-suppression
  • Malignancy
  • Diagnosis of Cushing’s syndrome
43
Q

Primary adrenal failure

Adrenal insufficiency

A

Primary adrenal failure

  • Hydrocortisone (10/5/5mg)
  • Fludrocortisone (100ug)
  • Mimic normal physiology
  • Fludrocortisone not in pituitary disease
44
Q

Inflammatory disease

A

Vasculitis

  • Sarcoidosis
  • Rheumatoid arthritis
  • Asthma

Gastro-intestinal disease

  • Inflammatory skin conditions
  • Nephrotic syndrome
  • Haematological conditions
  • Cerebral edema
45
Q

Immuno-suppression

A

Acute transplant rejection

  • Acute leukaemia
  • Pemphigus
  • Exfoliative dermatitis
46
Q

Malignancy

A
  • Hypercalcaemia
  • Improve appetite
  • Malignant oedem
47
Q

Diagnosis of Cushing’s syndrome

A

Dexamethasone suppression test

  • 2 days dexamethasone
  • Measure cortisol levels before and after
  • Normal individuals suppress < 50 nmol/l
  • Failure to suppress in Cushing’s syndrome
48
Q

Glucocorticoid side effect

A

Osteoporosis

  • Avascular necrosis
  • Peptic ulcers
  • Increased infections
  • Hypertension
  • Diabetes

Impaired growth

  • Skin atrophy
  • Cataracts
  • Corneal damage
  • Cushingoid features
49
Q

Cushingoid features

A

Rounded face

  • Plethoric features
  • Acne
  • Poor wound healing
  • Central obesity
  • Proximal myopathy

Buffalo hump

  • Thin skin
  • Easy bruising
  • Abdominal striae
  • Hypertension
  • Diabetes mellitus
50
Q

Adrenal suppression

A

Suppression of HPA axis occurs after 3 weeks

  • Prednisolone > 20mg will suppress HPA axis
  • May persist for years if long term treatment
  • Abrupt withdrawal may lead to hypo-adrenal crisis
51
Q

Hypoadrenal crisis

A
  • Hypotension
  • Hypoglycaemia
  • Hyponatraemia
  • Hyperkalaemia
  • Severe dehydration
  • Death if untreated
52
Q

Subtle symptoms of steroid withdrawal

A
  • Fever
  • Myalgia
  • Arthralgia
  • Weight loss
  • Conjunctivitis
  • Rhinitis
53
Q

Laparotomy or major procedure

A
  • Hydrocortisone 100mg IM at induction
  • Hydrocortisone 100mg IM 6 hourly until eating and drinking
  • Double normal dose oral steroids until full recovery
54
Q

Less invasive surgery

A

Hydrocortisone 100mg at time of procedure

• Double normal oral dose until full recovery

55
Q

‘Steroid sparing agents’

A
  • Reduced steroid requirement
  • Azathioprine
  • Cyclophosphamide
  • Biological therapies
  • Important for reducing steroid side effects

S6 (20 decks)

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