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Final Year MBBS > Pharmacology - Endocrinology > Flashcards

Pharmacology - Endocrinology Flashcards

1
Q

Metformin

A
  • *Indications:** ​Diabetes mellitus, PCOS
  • *MOA:** Biguanide: Insulin sensitiser → decreases gluconeogenesis, increases peripheral glucose use, decreases LDL and VLDL
  • *S/E’s:** Lactic acidosis, GI upset: N, V + D; anorexia/weight loss
  • *CI’s:** Caution in renal/hepatic impairment, heart failure, contrast media, general anaesthesia, recent MI, ketoacidosis
  • *Interactions:**
  • *Other info:** Renally excreted - reduce dose if renal impairment or avoid if GFR v.low. Cannot cause hypos
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2
Q

Pioglitazone

A
  • *Indications:** ​Type 2 DM (alone or combined with metformin or sulfonylurea)
  • *MOA:** Thiazolidinedione - peripheral insulin sensitiser, PPAR gamma ligand - a nuclear receptor involved in glucose and lipid homeostatsis
  • *S/E’s:** GI disturbance, weight gain, oedema, hepatotoxicity, may exacerbate HF
  • *CI’s:** Heart/liver failure, with insulin use or ACS
  • *Interactions:**
  • *Other info:** Very protein bound, hepatic metabolism therefore monitor LFTs
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3
Q

Sulfonylureas

Short acting –> Gliclazide, Tolbutamide, Glipizide

Long acting –> Glibenclamide

A
  • *Indications:** ​Type 2 DM
  • *MOA:** Sulfonylureas: insulin secretagogues –> block hyperpolarising K+ channel on beta cells –> depolarisation and insulin release
  • *S/E’s:** Hypoglycaemia - can be prolonged, weight gain, GI upset, headache
  • *CI’s:** Acute porphyria, severe liver/renal impairment
  • *Interactions:** Effects increased by: sulphonamides, trimethoprim, NSAIDs, warfarin, fibrates
  • *Other info:** Renally excreted; v. albumin bound; caution in elderly with reduced renal function; avoid long acting (glibenclamide) in the elderly
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4
Q

Nateglinide

Repaglinide

A
  • *Indications:** ​Type 2 DM in combination with metformin
  • *MOA:** Meglitinides - insulin secretagogues, block hyperpolarising K+ channels
  • *S/E’s:** Hypoglyaemia
  • *CI’s:** Ketoacidosis
  • *Interactions:**
  • *Other info:** Very short acting –> reduced risk of hypo; give before a meal
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5
Q

Exenatide

Liraglutide

A
  • *Indications:** ​Type 2 DM
  • *MOA:** Insulin secretagogue: GLP-1 analogue –> increased insulin secretion and sensitisation
  • *S/E’s:** GI upset; hypoglycaemia
  • *CI’s:** Ketoacidosis, severe GIT disease
  • *Interactions:**
  • *Other info:** Give by SC injection
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6
Q

Sitagliptin

Vildagliptin

A

Indications: ​​Type 2 DM
MOA: Insulin secretagogues: dipeptidylpeptidase-4 inhibitor, DPP-4 breaks down endogenous GLP-1
S/E’s: GI upset, hypoglycaemia
CI’s: Ketoacidosis, discontinue if signs of severe acute pancreatitis
Interactions:
Other info:

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7
Q

Acarbose

A

Indications: ​DM inadequately controlled by diet
MOA: Intestinal alpha-glucosidase inhibitor: delays carb absorption –> decreases post prandial blood glucose. Little effect on fasting glucose
S/E’s: Flatulence, loose stools/diarrhoea, abod pain, bloating, hepatotoxicity (rare)
CI’s: IBD, liver impairment
Interactions:
Other info: Monitor LFTs

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8
Q

Levothyroxine

A

Indications: ​Hypothyroidism
MOA: Synthetic form of thyroxine
S/E’s: Precipitation of HF, osteopenia, AF. Over Rx –> hyperthyroidism
CI’s: Thyrotoxicosis; caution in elderly, cardio disorders e.g. HTN, MI etc
Interactions:
Other info: In the elderly start low and go slow

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9
Q

Carbimazole

Propythiouracil (PTU)

A

Indications: ​Hyperthyroidism
MOA: Thionamides - thyroperoxidase inhibitors, prevent iodination of tyrosine = reduced T4/T3 synthesis. Carbimazole is a pro-drug converted to methimazole
S/E’s: Hypersensitivity, hepatitis, GI disturbance, agranulocytosis - often transient and benign
CI’s: Severe blood disorders. Use PTU in pregnancy and children. If there is tracheal compression do sx
Interactions:
Other info: PTU reserved for those intolerant of carbimazole due to it’s increased risk of hepatitis. Titrate to normal TSH or use a block and replace regime

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10
Q

Radioiodine: I131

A

Indications: ​Thyrotoxicosis
MOA: Radioiodine is localised to the thyroid causing gland destruction
S/E’s: Hypothyroidism = need lifelong levothyroxine. Can precipitate a thyroid storm
CI’s:
Interactions:
Other info: Stop thionamide before use

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11
Q

Dopamine agonists

Short acting: Bromocriptine

Long acting: Cabergoline, Pergolide

A
  • *Indications: ​**Galactorrhoea, prolactinomas (Parkinson’s) Bromocriptine also inhibits GH so can be used for acromegaly
  • *MOA:** Ergot-derived DA agonists
  • *S/E’s:** Fibrosis, GI upset, nausea, postural hypotension, drowsiness, neuropsych syndromes e.g. dyskinesia
  • *CI’s:** CVS disease, prophyria, psychosis
  • *Interactions:** Levels increased by: octreotide, macrolides, dobutamine
  • *Other info:** Monitor heart with echo
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12
Q

Octreotide

Lanreotide

Somatostatin analogues

A
  • *Indications: ​**Acromegaly, Carcinoid syndrome
  • *MOA:** Somatostatin analogues
  • *S/E’s:** Diarrhoea, gallstones
  • *CI’s:** Monitor TFTs + LFTs
  • *Interactions:** Decreased requirement for antidiabetics
  • *Other info:** Octreotide = TDS, Lanreotide = monthly
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13
Q

Pegvisomant

A

Indications: ​Acromegaly
MOA: GH receptor antagonist
S/E’s: GI upset, raised LFTs
CI’s: Caution in liver disease + DM
Interactions:
Other info:

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14
Q

Metyrapone

A

Indications: ​Can be used in Cushing’s syndrome that is not amenable to surgery, also used pre-surgery
MOA: Competitive inhibitor of 11-beta-hydroxylase in the adrenal cortex–> results in the inhibition of cortisol (+ to some extent aldosterone) production
S/E’s: GI upset, dizziness, headache
CI’s: Adrenocortical insufficiency, use with caution in hepatic impairment
Interactions:
Other info:

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15
Q

Cinacalcet

A

Indications: ​Secondary hyperparathyroidism in ESRF, can also use in 1º hyperPTH or parathyroid carcinoma
MOA: Calcimimetic → decreased PTH secretion
S/E’s: N+V, dizziness
CI’s: Measure serum Ca before starting Rx then monitor during Rx. Caution in mod-severe hepatic impairment
Interactions:
Other info:

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16
Q

Sevelamer

Lanthanum

A

Indications: ​Hyperphosphataemia in Pts’ on haemo- or peritoneal dialysis
MOA: Phosphate binder
S/E’s: N+V, abdo pain, constipation/diarrhoea
CI’s: Bowel obstruction, caustion in GI disorders
Interactions:
Other info:

17
Q

Alendronate

Etidronate

Pamidronate

Zoledronate

A

Indications: ​Prophylaxis and Rx of OP and osteoporotic #, Paget’s disease of the bone, hypercalcaemia of malignancy and bone mets in breast cancer
MOA: Bisphosphonates → absorbed onto hydroxyapatite crystals in bone, clowing both their rate of growth and dissolution thus decrease the rate of bone turnover
S/E’s: Oesophagitis and ulcers, abdo pain, MSK pain, GI upset, osteonecrosis of the jaw
CI’s: Abnormalities of the oesophagus e.g. achalasia, oesophageal stricture
Interactions:
Other info: Take with a glass of water on an empty stomach 30 mins before breakfast, staying upright

18
Q

Strontium

A

Indications: ​Severe postmenopausal OP in women at high risk of # (or men with high risk of #)
MOA: Stimulates bone formation and decreases bone resorption
S/E’s: Increased risk of serious cardiovascular disease including MI → assess risk before Rx
DRESS syndrome: drug rash eosinophilia systemic symptoms (fever, high WCC)
CI’s: Current or previous VTE, IHD, PAD(PVD), CVD, uncontrolled HTN
Interactions:
Other info:

19
Q

Teriparatide

A

Indications: ​Treatment of OP in postmenopausal women + men at high risk of #
MOA: Recombinant PTH which when given in pulses increases bone formation and decreases resorption
S/E’s: GI upset
CI’s: Pre-existing hypercalcaemia, skeletal malignancies or bone mets, metabolic bone disease, severe renal failure
Interactions:
Other info:

20
Q

Denosumab

A

Indications: ​Prevention of osteoporotic #s in postmenopausal women
MOA: Monoclonal Ab = anti-RANKL → inhibits osteoclast formation, function and survival thus decreases bone resorption
S/E’s: GI upset, UTI, URTI
CI’s: Correct hypocalcaemia and vit D deficiency before starting
Interactions:
Other info: Used if bisphosphonates not tolerated

21
Q

Ergocalciferol

A

Indications: ​Vitamin D deficiency
MOA: Vitamin D2
S/E’s: Symptoms of OD = anorexia, N+V, diarrhoea/constipation etc.
CI’s: Hypercalaemia, metastatic calcification
Interactions:
Other info:

22
Q

Colecalciferol

A

Indications: ​Vitamin D deficiency
MOA: Vitamin D3
S/E’s: Symptoms of OD = anorexia, N+V, diarrhoea/constipation etc.
CI’s: Hypercalcaemia, metastatic calcification
Interactions:
Other info:

23
Q

Alfacalcidol

A

Indications: ​Vitamin D deficiency in those with severe renal impairment
MOA: 1α (OH) Vit D3 → already hyroxylated so doesn’t need the kidney
S/E’s: Symptoms of OD = anorxia, N+V, diarrhoea/constipation etc.
CI’s: Hypercalaemia, metastatic calcification
Interactions:
Other info:

24
Q

Calcitriol

A

Indications: ​Vit D deficiency in those with severe renal impairment
MOA: 1,25(OH)Vit D3 = active form
S/E’s: Symptoms of OD = anorexia, H+V, diarrhoea/constipation etc.
CI’s: Hypercalcaemia, metastatic calcification
Interactions:
Other info:

25
Q

Raloxifene

A

Indications: ​Treatment and prevention of postmenopausal osteoporosis
MOA: SERM
S/E’s: Hot flushes, leg cramps, peripheral oedema
CI’s: Hx of VTE, endometrial cancer, cholestasis
Interactions:
Other info:

26
Q

COCP

A
  • *Indications: ​**Contraception, dysmenorrhoea, menorrhagia, PMT. Reduces risk of benign breast disease, ovarian + endometrial Ca, and PID
  • *MOA:** Combined hormones, prevents ovulation
  • *S/E’s:** Increased risk of VTE, small increased risk of breast Ca + IHD, gall stones, cholestatic jaundice, breast tenderness, hepatoma
  • *CI’s:** Personal Hx of VTE, high risk of VTE, high risk of stoke + IHD, Hx of breast Ca
  • *Interactions:** P450 metabolism: reduced effectiveness with enzyme inducers. Increases the effects of steroids
  • *Other info:** Don’t need extra contraception when taken with oral Abx that don’t induce liver enzymes, unless D+V
27
Q

POP

A
  • *Indications: ​**Contraception esp in those who cannot take the COCP
  • *MOA:** Progesterone only
  • *S/E’s:** N+V, headache, increased weight, breast tenderness
  • *CI’s:** Severe arterial disease, Hx of breast Ca
  • *Interactions:** P450 metabolism: reduced effectiveness with enzyme inducers
  • *Other info:**
28
Q

HRT

A

Benefits: ​↓ hot flushes, ↓ vaginal dryness, ↑libido, ↓ urinary frequency / urgency, ↓ risk of bowel Ca, ↓ risk of osteoporotic #s
MOA: Hormone replacement
S/E’s: Increased risk of breast, endometrial + ovarian cancer, increased risk of VTE, stroke + IHD, cholestatic jaundice
CI’s: Oestrogen dependent cancer, Hx of breast cancer, undiagnosed vaginal bleeding, VTE
Interactions:
Other info: Excess Ca risk disappears within 5 years of stopping

29
Q

Testosterone:

restandol (oral)
sustanon (IM)
andropatch (transdermal)

A
  • *Indications:** male androgen deficiency
  • *MOA:**
  • *SE’s:** Androgenic effects e.g. hirsutism, acne, balness. Prostate enlargement, cholestatic jaundice
  • *CI’s:** Some cancers e.g. liver, prostate
  • *Interaction:** Potentiates warfarin
  • *Other:**

Final Year MBBS (39 decks)

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