Pharmacology Flashcards
1
Q
is biliary excreted so it is safe for renal impairment patients
A
indapamide, clopamid, Xipamide
2
Q
they are Ca channel blockers and Diuretics
A
Indapamide, Clopamide, Xipamide
3
Q
is effective in renal impairment if GFR is 20ml/min
A
Metolazone
4
Q
short acting thiazide
A
cloro, Hydrocloro, Hydroflumme, bendroflumme
5
Q
Long acting thiazide
A
Cyclo, poly, thriclormethiazide
6
Q
the only thiazide drug that taken parenteral
A
chlorothiazide
7
Q
thiazide taken?
A
orally
8
Q
which tubule is thiazide secreted
A
actively secreted in PCT
9
Q
antagonized with thiazide diuretic effect
A
Probenecid
تيته مينفعش تاخد دوا النقرس مع دوا البول
10
Q
used in nephrogenic diabetes insipidus
A
thiazide
act as antidiuretic, it increases ADH sensitivity
11
Q
Therapeutic uses of Thiazide
A
- Edema (renal, hepatic, cardiac)
- mild to moderate hypertension
- nephrogenic diabetes insipidus
- premenstrual tension and migraine
- Calcinuria, Ca renal stones, hypocalcemia, osteoporosis
12
Q
Diuretic that is safe to renal impairment patients
A
indapamide, Xipamide, Chlopamide
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
14
Q
Results of thiazide in blood
A
Hypovolemia
Hyponatrimea
Hypokalemia
Hypochloremia
Hypomagnesmia
alkalosis
Hypercalcemia
15
Q
what happens to thiazide effectivity when GFR less than 20ml/min
A
losses in diuretic effect
16
Q
the effect of thiazide in nephrogenic Diabetes insipidus
A
act as antidiuretic by increase the sensitivity of ADH by the kidney
17
Q
the effects of the thiazide
A
- Diuretic effect
- Antidiuretic effect in Diabetes insipidus
- Antihypertensive
- Hyperglycemia
- Hyperlipidemia
- Hyperuricemia
18
Q
How thiazide make its antihypertensive effect
A
By its diuretic effect and direct VD
19
Q
What the thiazide make in VD
A
- it is a K channel opener that leads to hyperpolarization
- it secretes prostaglandins. NSAIDs decrrease its effect
- it decreases Na load and edema in BV so decreases the effect of adrenaline and angiotensin
20
Q
how thiazide cause hyperglycemia?
A
it is a K channel opener and decrease insulin secretion from panceas
21
Q
How thiazide cause hyperuricemia
A
it competes with uric acid in secretion
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
23
Q
Adverse effects of thiazide
A
- Hypovolemia
- Hyponatremia
- Hypokalemia
- Hypochloremia
- Hypomagnesmia
- Alkalosis
- Hypercalcemia
- hyperglycemia
- hyperlipidemia
- hyperuricemia
- Allergy and cross allergy
- GIT irritation
- Bone marrow depression
- Fetotoxicity
24
Q
Contraindications of thiazide and frusemide
A
- hypersensitivity
- Pregnancy
- Gout
- renal and hepatic insufficiency
- Diabetes mellitus
- with digitalis
- with steroids (more worsening of hypokalemia)
25
causes Hyperammonemia
Acetazolamide
26
Causes Fetotoxicity
Thiazide and Frusemide
| because it passes placenta
27
Theraputic uses of Acetazolamide
1. Edema
2. Glucoma
3. petit mal epilepsy
4. alkalinize urine to dissolve urate stones
5. prevention of acute mountain sickness
28
side effects of Acetazolamide
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
29
Sulfonamide derivatives of loop diuretics
Frusemide, Torsemide, Bumetanide
30
Non- sulfonamide derivatives of loop diuretics
Ethacrynic acid, Idocrinone, Tienilic acid
31
absorption of loop diuretics
oral and IV
32
uses extensive plasma protein binding
loop diuretics
33
where is loop secreted
PCT
34
Frusemide
oral onset of action .... min and ..... h duration
IV onset of action .... min and .... h duration
30 min -- 6 h
2-5 min ----- 3h
35
needs hepatic metabolism
loop
36
needs hepatic metabolism
loop
Spironolactone
37
inhibit carbonic anhydrase enzyme
acetazolamide
frusemide
38
mechanism of action of Fursemide
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
39
effect of loop on blood
1. hypovolemia
2. hyponatrimia
3. hypokalemia
4. hypochloremia
5. alkalosis
6. hypomagnesmia
7. hypocalcemia
40
effective as diuretic even if GFR less than 10 ml / min
Frusemide
41
has antihypertensive effect: Only by its diuretic effect. No direct VD effect.
Frusemide
42
actions of Frusemide
diuretic effect
antihypertensive effet
hyperglycemia
hyperlipidemia
hyperuricemia
43
increase protaglandins secretion
thiazide
frusemide
44
used in cerebral edema
Frusemide given IV
45
best in acute heart failure (pulmonary edema)
Frusemide
46
best in sever or refractory edema
Frusemide>>thiazide
47
Uses of Frusemide
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
used to emergency hypertension as in hypertensive encephalopathy
Frusemide given IV
49
best in acute renal impairment
Frusemide
50
used in hypercalcemia
Frusemide
51
side effects of Frusemide different of thiazide
1. hypocalcemia
2. renal caliculi
3. Nephrotoxicity: intersitial nephritis
4. ototoxicity specially in patient with renal impairment or using ototoxic drugs gentamycin
52
Drug interactions of Frusemide
1. warfarin
2. lithium carbonate
3. Probencid
4. NSAIDS
5. Aminoglycosides
6. Cephalosporins
7. Digitalis
53
have more potent diuretic effect than Frusemide
Torsemide and Bumetanide
54
has the same efficacy of frusemide, but it has direct VD effect.
Piretanide
55
non sulfa loops different from frusemide in
1. non sulfa ( not inhibit carbonic anhydrase, no cross allergy)
2. uricosuric effect
3. more irritating to GIT
4. cause sever deafness
56
mannitol is given by
IV
57
used in acute glaucoma
mannitol
58
used in increased intracranial tension
mannitol
59
used in chronic glaucoma
Glycerol
60
osmotic diuretics
1. mannitol
2. urea
3. glucose
4. glycerol
61
from loop diuretics has uricosuric effect
Ethacrynic acid, indacrinone, tiellnic acid
62
Aldosterone antagonists
spironolactone and eplerenone
| Aldo spiro Eple
63
Non-Aldosterone antagonists
amiloride and triamterene
64
source of spironolactone
synthetic
65
chemistry of spironlactone
steroid
66
pharmokinetics of spironolactone
* absorbed orally
* converted in liver to canrenone
* delayed onset and long duration
* pass BBB
67
mechanism of action of spironolactone
antagonizes aldosterone for mineralcorticoid receptors in DCT and collecting ducts leading to inhibition of Na/k exchanger and Na/H exchanger
68
pharmacological actions of spirono
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
used in hyperaldosteronism
spironolactone
70
uses of sprironolactone
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
used in conn's syndrome
spironolactone
72
causes sexual disturbance
spironolactone
73
adverse effects of spironlactone
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
similar to spironolactone but without sexual disturbance side effects
Eplerenone
75
Drug interactions of spironolactone
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
used in lithium-induced nephrogenic diabetes insipidus.
amiloride
77
causes hypersensitivity as photosensitivity
amiloride and triamterene
78
causes skin rash
spironolactone
79
adverse effects of non aldosterone antagonizes
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
unmask the nephrotoxic effect of triamterene
indamethacin
81
from acidyfing diuretics
ammonium chloride
82
causes hyperchloremic acidosis
ammonium chloride
83
causes acidic urine
ammonium chloride
84
used as nauseant expectorant
Ammonium chloride
85
Treat hypocalcemia and tetany
Ammonium chloride
86
increase excretion of basic drugs as amphetamine and ephedrine
Ammonium chloride
87
causes acidosis and acidic urine
Ammonium chloride
88
increase activity of urinary antiseptic such as methenamine
Ammonium chloride
89
treat tetany
Ammonium chloride
90
Urine alkalinizers
Na bicarbonate, lactate, acetate
91
uses of methylxanthine
acute pulmonary edema
92
action of Theophylline
decrease NaCl reabsorption and increase excretion with water in urine
93
uses of urine alkalinzers
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
help excretion of acidic drugs as aspirin and penicillin
urine alkalinzers (Na bicarbonate, lactate, acetate)
95
relieve dysuria and inhibit growth of E-coli in UTI.
urine alkalinzers
96
used as Alkaline expectorants.
urine alkalinzers
97
To increase activity of sulphonamide and prevent formation of renal stones by sulfa.
urine alkalinzers
98
causes hepatic encephalopathy
acetazolamide
| due to hyperammonemia
99
Drugs that can cause hyperuricemia
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
xanthine oxidase inhibitors
Allopurinol
101
Mechanism of Action of colchicine
1. Selective inhibitor of microtubule assembly →↓ leucocyte migration & phagocytosis.
2. Reduces production of leukotriene B4 (chemotactic for neutrophils).
102
contraindicated in patients with G6PD deficiency
pegloticase
103
They are similar to thiazide pharmacologically but differ chemically
with long duration of action
1. Chlorothaldione
2. Indapamide, Clopamide and Xipamide
3. Metolazone
104
acetazolamide given?
oral, IV, eye drops
105
f
106
f
107
other urine acidifier
Ascorbic acid and methionine
108
causes Hyperchloremic acidosis
Acetazolamide
ammonium chloride (acidifying diuretic)
109
uricosuric drugs
Probenecid - Sulfinpyrazone - Benzbromarone
110
Mechanism of uricosuric drugs
Directly inhibit URAT-1 (a urate-anion exchanger located at the apical brush border of the proximal nephron) and therefore, reduce urate reabsorption
