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2nd Year Adrenergic Blockers > Pharmacology > Flashcards

Pharmacology Flashcards

1
Q

is biliary excreted so it is safe for renal impairment patients

A

indapamide, clopamid, Xipamide

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2
Q

they are Ca channel blockers and Diuretics

A

Indapamide, Clopamide, Xipamide

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3
Q

is effective in renal impairment if GFR is 20ml/min

A

Metolazone

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4
Q

short acting thiazide

A

cloro, Hydrocloro, Hydroflumme, bendroflumme

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5
Q

Long acting thiazide

A

Cyclo, poly, thriclormethiazide

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6
Q

the only thiazide drug that taken parenteral

A

chlorothiazide

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7
Q

thiazide taken?

A

orally

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8
Q

which tubule is thiazide secreted

A

actively secreted in PCT

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9
Q

antagonized with thiazide diuretic effect

A

Probenecid

تيته مينفعش تاخد دوا النقرس مع دوا البول

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10
Q

used in nephrogenic diabetes insipidus

A

thiazide

act as antidiuretic, it increases ADH sensitivity

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11
Q

Therapeutic uses of Thiazide

A
  1. Edema (renal, hepatic, cardiac)
  2. mild to moderate hypertension
  3. nephrogenic diabetes insipidus
  4. premenstrual tension and migraine
  5. Calcinuria, Ca renal stones, hypocalcemia, osteoporosis
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12
Q

Diuretic that is safe to renal impairment patients

A

indapamide, Xipamide, Chlopamide

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13
Q

Mechanism of Action of Thiazide

A

1) thiazide actively secreted in PCT ana Probenecid antagonizes its Diuretic effect
2) thiazide act in early part of DCT by inhibiting Na/Cl symporter and reabsorption (only 10% of Na)
3) excess Na reaches late part of DCT which exchanged with K and H
4) the remaining is secreted in urine with water

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14
Q

Results of thiazide in blood

A

Hypovolemia
Hyponatrimea
Hypokalemia
Hypochloremia
Hypomagnesmia
alkalosis
Hypercalcemia

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15
Q

what happens to thiazide effectivity when GFR less than 20ml/min

A

losses in diuretic effect

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16
Q

the effect of thiazide in nephrogenic Diabetes insipidus

A

act as antidiuretic by increase the sensitivity of ADH by the kidney

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17
Q

the effects of the thiazide

A
  1. Diuretic effect
  2. Antidiuretic effect in Diabetes insipidus
  3. Antihypertensive
  4. Hyperglycemia
  5. Hyperlipidemia
  6. Hyperuricemia
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18
Q

How thiazide make its antihypertensive effect

A

By its diuretic effect and direct VD

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19
Q

What the thiazide make in VD

A
  1. it is a K channel opener that leads to hyperpolarization
  2. it secretes prostaglandins. NSAIDs decrrease its effect
  3. it decreases Na load and edema in BV so decreases the effect of adrenaline and angiotensin
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20
Q

how thiazide cause hyperglycemia?

A

it is a K channel opener and decrease insulin secretion from panceas

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21
Q

How thiazide cause hyperuricemia

A

it competes with uric acid in secretion

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22
Q

how thiazide is useful in heart failure

A

it causes diuresis so it decreases reduces return and EDV and decreases preload
It is direct arterial VD thus reduces afterload

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23
Q

Adverse effects of thiazide

A
  1. Hypovolemia
  2. Hyponatremia
  3. Hypokalemia
  4. Hypochloremia
  5. Hypomagnesmia
  6. Alkalosis
  7. Hypercalcemia
  8. hyperglycemia
  9. hyperlipidemia
  10. hyperuricemia
  11. Allergy and cross allergy
  12. GIT irritation
  13. Bone marrow depression
  14. Fetotoxicity
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24
Q

Contraindications of thiazide and frusemide

A
  1. hypersensitivity
  2. Pregnancy
  3. Gout
  4. renal and hepatic insufficiency
  5. Diabetes mellitus
  6. with digitalis
  7. with steroids (more worsening of hypokalemia)
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25
Q

causes Hyperammonemia

A

Acetazolamide

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26
Q

Causes Fetotoxicity

A

Thiazide and Frusemide

because it passes placenta

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27
Q

Theraputic uses of Acetazolamide

A
  1. Edema
  2. Glucoma
  3. petit mal epilepsy
  4. alkalinize urine to dissolve urate stones
  5. prevention of acute mountain sickness
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28
Q

side effects of Acetazolamide

A
  1. weak and self limiting Diuretic
  2. Allergy and Cross allrgy
  3. metabolic acidosis
  4. alkaline urine leads to formation of phosphate stones
  5. Hepatic encephalpathy in patient with hepatic insufficinecy due to hyperammonemia
  6. CNS sedation and drowsiness
  7. Hypokalemia
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29
Q

Sulfonamide derivatives of loop diuretics

A

Frusemide, Torsemide, Bumetanide

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30
Q

Non- sulfonamide derivatives of loop diuretics

A

Ethacrynic acid, Idocrinone, Tienilic acid

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31
Q

absorption of loop diuretics

A

oral and IV

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32
Q

uses extensive plasma protein binding

A

loop diuretics

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33
Q

where is loop secreted

A

PCT

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34
Q

Frusemide
oral onset of action …. min and ….. h duration
IV onset of action …. min and …. h duration

A

30 min – 6 h
2-5 min —– 3h

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35
Q

needs hepatic metabolism

A

loop

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36
Q

needs hepatic metabolism

A

loop
Spironolactone

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37
Q

inhibit carbonic anhydrase enzyme

A

acetazolamide
frusemide

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38
Q

mechanism of action of Fursemide

A
  1. fursemide is actively secreted in PCT. Probenecid antgonizes its diuretic effect
  2. Fursemide has sulfa radical that inhibit carbonic anhydrase enzyme
  3. Frusemide act in the thick part of ascending loop of Henle by inhibition of symporter Na/k/Cl that disturb countercurrent multiplier system leads to excess water excretion.
  4. excess Na is go to DCT and some of them exchanged with K and H
  5. the remaining is excreted with water
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39
Q

effect of loop on blood

A
  1. hypovolemia
  2. hyponatrimia
  3. hypokalemia
  4. hypochloremia
  5. alkalosis
  6. hypomagnesmia
  7. hypocalcemia
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40
Q

effective as diuretic even if GFR less than 10 ml / min

A

Frusemide

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41
Q

has antihypertensive effect: Only by its diuretic effect. No direct VD effect.

A

Frusemide

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42
Q

actions of Frusemide

A

diuretic effect
antihypertensive effet
hyperglycemia
hyperlipidemia
hyperuricemia

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43
Q

increase protaglandins secretion

A

thiazide
frusemide

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44
Q

used in cerebral edema

A

Frusemide given IV

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45
Q

best in acute heart failure (pulmonary edema)

A

Frusemide

46
Q

best in sever or refractory edema

A

Frusemide»thiazide

47
Q

Uses of Frusemide

A
  1. Edema (pulmonary edema from acute left sided heart failure,, cerebral edema given IV, sever edema)
  2. hypertension
    emergency hypertension and hypertensive encephalopathy by IV
    sever or resistant HTN given oral
    hypertension with renal impairment
  3. acute renal failure
  4. Hypercalcemia
  5. hyperkalemia
48
Q

used to emergency hypertension as in hypertensive encephalopathy

A

Frusemide given IV

49
Q

best in acute renal impairment

A

Frusemide

50
Q

used in hypercalcemia

A

Frusemide

51
Q

side effects of Frusemide different of thiazide

A
  1. hypocalcemia
  2. renal caliculi
  3. Nephrotoxicity: intersitial nephritis
  4. ototoxicity specially in patient with renal impairment or using ototoxic drugs gentamycin
52
Q

Drug interactions of Frusemide

A
  1. warfarin
  2. lithium carbonate
  3. Probencid
  4. NSAIDS
  5. Aminoglycosides
  6. Cephalosporins
  7. Digitalis
53
Q

have more potent diuretic effect than Frusemide

A

Torsemide and Bumetanide

54
Q

has the same efficacy of frusemide, but it has direct VD effect.

A

Piretanide

55
Q

non sulfa loops different from frusemide in

A
  1. non sulfa ( not inhibit carbonic anhydrase, no cross allergy)
  2. uricosuric effect
  3. more irritating to GIT
  4. cause sever deafness
56
Q

mannitol is given by

A

IV

57
Q

used in acute glaucoma

A

mannitol

58
Q

used in increased intracranial tension

A

mannitol

59
Q

used in chronic glaucoma

A

Glycerol

60
Q

osmotic diuretics

A
  1. mannitol
  2. urea
  3. glucose
  4. glycerol
61
Q

from loop diuretics has uricosuric effect

A

Ethacrynic acid, indacrinone, tiellnic acid

62
Q

Aldosterone antagonists

A

spironolactone and eplerenone

Aldo spiro Eple

63
Q

Non-Aldosterone antagonists

A

amiloride and triamterene

64
Q

source of spironolactone

A

synthetic

65
Q

chemistry of spironlactone

A

steroid

66
Q

pharmokinetics of spironolactone

A
  • absorbed orally
  • converted in liver to canrenone
  • delayed onset and long duration
  • pass BBB
67
Q

mechanism of action of spironolactone

A

antagonizes aldosterone for mineralcorticoid receptors in DCT and collecting ducts leading to inhibition of Na/k exchanger and Na/H exchanger

68
Q

pharmacological actions of spirono

A

increase Na, Cl, Ca, water in urine (low efficacy)
k retention leading to hyperkalemia
H retention leading to acidosis and alkalinization of urine
No hyperglycemia
No hyperlipidemia
No hyperuricemia

69
Q

used in hyperaldosteronism

A

spironolactone

70
Q

uses of sprironolactone

A

achieve synergism by using it with thiazide or loop diuretics to save K
alternatives to thiazide and loop diuretics when the are contraindicated
used in hyperaldosteronism which is either primary conn’s syndrome ore secondary to liver cirrhosis, nephrotic syndrome, and congestive heart
failure

71
Q

used in conn’s syndrome

A

spironolactone

72
Q

causes sexual disturbance

A

spironolactone

73
Q

adverse effects of spironlactone

A

Hyperkalemia specially with renal impairment
acidosis
hypersensitivity reactions
Gut upset: gastritis, diarrhea, gastric bleeding
CNS disturbance: headache, drowsness, confusion
Feminzation (gunecomastia) and impotence in males and irregular menstruation and musculization in females

74
Q

similar to spironolactone but without sexual disturbance side effects

A

Eplerenone

75
Q

Drug interactions of spironolactone

A
  1. with thiazide and loop diuretics caues synergism and saves K
  2. with ACE inhibitors, AT antagonist, b- blocker, NSAID leads to sever hyperkalemia
  3. Carbenoxolone
76
Q

used in lithium-induced nephrogenic diabetes insipidus.

A

amiloride

77
Q

causes hypersensitivity as photosensitivity

A

amiloride and triamterene

78
Q

causes skin rash

A

spironolactone

79
Q

adverse effects of non aldosterone antagonizes

A
  1. hyperkalemia
  2. acidosis
  3. photosensitivity
  4. Gut upset
  5. Triamterene causes renal stones and acute renal failure if given with prostaglandins inhibitors as indomethacin
80
Q

unmask the nephrotoxic effect of triamterene

A

indamethacin

81
Q

from acidyfing diuretics

A

ammonium chloride

82
Q

causes hyperchloremic acidosis

A

ammonium chloride

83
Q

causes acidic urine

A

ammonium chloride

84
Q

used as nauseant expectorant

A

Ammonium chloride

85
Q

Treat hypocalcemia and tetany

A

Ammonium chloride

86
Q

increase excretion of basic drugs as amphetamine and ephedrine

A

Ammonium chloride

87
Q

causes acidosis and acidic urine

A

Ammonium chloride

88
Q

increase activity of urinary antiseptic such as methenamine

A

Ammonium chloride

89
Q

treat tetany

A

Ammonium chloride

90
Q

Urine alkalinizers

A

Na bicarbonate, lactate, acetate

91
Q

uses of methylxanthine

A

acute pulmonary edema

92
Q

action of Theophylline

A

decrease NaCl reabsorption and increase excretion with water in urine

93
Q

uses of urine alkalinzers

A

1- Alkaline expectorants.
2- Treat metabolic acidosis.
3- Alkalinize urine:
a. To increase excretion of acidic drugs as aspirin and penicillin.
b. To relieve dysuria and inhibit growth of E-coli in UTI.
c. To increase activity of sulphonamide and prevent formation of renal
stones by sulfa.
d. To dissolve urate renal stones

94
Q

help excretion of acidic drugs as aspirin and penicillin

A

urine alkalinzers (Na bicarbonate, lactate, acetate)

95
Q

relieve dysuria and inhibit growth of E-coli in UTI.

A

urine alkalinzers

96
Q

used as Alkaline expectorants.

A

urine alkalinzers

97
Q

To increase activity of sulphonamide and prevent formation of renal stones by sulfa.

A

urine alkalinzers

98
Q

causes hepatic encephalopathy

A

acetazolamide

due to hyperammonemia

99
Q

Drugs that can cause hyperuricemia

A

Aspirin: small dose competes with uric acid for acid secretory system.
Diuretics: competes with uric acid for organic acid secretory system.
Alcohol: ↑ urate production (↑nucleotides catabolism) - ↓ urate excretion.
Cytotoxics: ↑ uric acid production (↑ nucleic acid turnover).

100
Q

xanthine oxidase inhibitors

A

Allopurinol

101
Q

Mechanism of Action of colchicine

A
  1. Selective inhibitor of microtubule assembly →↓ leucocyte migration & phagocytosis.
  2. Reduces production of leukotriene B4 (chemotactic for neutrophils).
102
Q

contraindicated in patients with G6PD deficiency

A

pegloticase

103
Q

They are similar to thiazide pharmacologically but differ chemically
with long duration of action

A
  1. Chlorothaldione
  2. Indapamide, Clopamide and Xipamide
  3. Metolazone
104
Q

acetazolamide given?

A

oral, IV, eye drops

105
Q

f

A
106
Q

f

A
107
Q

other urine acidifier

A

Ascorbic acid and methionine

108
Q

causes Hyperchloremic acidosis

A

Acetazolamide
ammonium chloride (acidifying diuretic)

109
Q

uricosuric drugs

A

Probenecid - Sulfinpyrazone - Benzbromarone

110
Q

Mechanism of uricosuric drugs

A

Directly inhibit URAT-1 (a urate-anion exchanger located at the apical brush border of the proximal nephron) and therefore, reduce urate reabsorption

2nd Year Adrenergic Blockers (12 decks)

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