mcq Flashcards
1
Q
caues allergic obstructive cholestatic jaundice
A
chloropromazine
2
Q
not cns adverse effect of choropromazine
A
2-Increased body weight.
3- Opacities of cornea and lens.
4- Dry mouth
5- Allergy: Dermatitis, photosensitivity & Agranulocytosis.
6- Tachycardia.
7- Endocrine disturbances e.g. Gynecomastia & galactorrhea.
8- Allergic obstructive cholestatic jaundice.
9- Teratogenic, so not used in vomiting of pregnancy.
10- Postural hypotension.
3
Q
side effects of thioredazine
A
Similar to Chlorpromazine + Cardiotoxic & Retinopathy.
4
Q
Phenothiazine causes cardiotoxic and retinopathy side effect
A
Thioridazine
5
Q
More effective in treatment of negative symptoms of schizophrenia with Less side effects.
A
Atypical (2™ generation) Anti-Psychotic Drugs
6
Q
Atypical (2™ generation) Anti-Psychotic Drugs
A
Sulpiride
Clozapine
Risperidone
Olanzapine
Quetiapine
Aripiprazole
Pimozide
7
Q
Pharmacodynamics of fluoxetine
A
- Antidepressant Effect: Elevate mood in depressed patients by selective block of serotonin uptake by nerve endings
- The Antidepressant Effect appears after 2-3 WEEKS and lasts for 2-3 WEEKS after stop of SSRI
8
Q
Therapeutic Uses
A
Psychic depression
panic disorders
Obsessive compulsive disorders (better than the TCA clomipramine).
Eating disorders {Bulimia nervosa} » Ineffective in anorexia nervosa
Post-traumatic stress disorder
Premenstrual syndrome — for 2 weeks in Iuteal phase
Premature ejaculation
9
Q
Adverse Effects of Fluoxetine
A
- Anorexia, nausea & diarrhea — Due to Increased serotonin in GIT
b- Headache, insomnia, hypersomnia.
c- Weight gain
d- Increases aggression, violence & suicide.
e- Category C in pregnancy — Give if benefits outweigh the risk
d- Fluoxetine + MAQOI — Serotonin syndrome (May be FATAL)— Accumulation of
serotonin »Reduced neuronal uptake (SSRI) + Reduced metabolism (MAOI) # Triad of
cognitive (delirium), autonomic (hypertension and tachycardia), and somatic
manifestations (tremors and myoclonus)
+ Stop fluoxetine 4-56 weeks before initiating MAOIs
10
Q
contraindication of fluoxetine
A
bipolar depression
11
Q
non TCA useful in urinary incontinence and anxiety disorders
A
Duloxetine
12
Q
Synthetic form of the ma or active metabolite of venlafaxine
A
desvenlafaxine
13
Q
manage fibromyalgia and mention its family
A
milnacipran
non TCA selective na/5HT Reuptake inhibitors
14
Q
Inhibits NA and dopamine uptake
Slow release formulations help in cessation of smoking
A
Buprion
15
Q
for managment of ADHD
A
Atomexetine
reboxetine
16
Q
Blocks alpha-2, 5-HT3, 5-HT2C receptors release of NA and -HT
A
mirtazepine
17
Q
Blocks 5-HT2A, 5-HT2C receptors ( release of NA and 5-HT) and H1 receptors
A
Trazodone
18
Q
adverse effect of MAO inhibitors
A
1- Cheese Reaction (NOT with Moclobemide or Selegiline): Eating or drinking foods
that contain TYRAMINE or DOPA such as Aged cheese, Broad beans, Soy products, or
Yogurt — Malignant Hypertension — Stroke and myocardial infarction.
2- -DOPA(Anti-Parkinsonian) — Agitation & Hypertension.
3-Potentiates Indirectly Acting Sympathomimetics e.g. Amphetamine.
1- Avoid over-the -counter flu medications as they contain sympathomimetics
e.g. pseudoephedrine
5- SSRI (Fluoxetine), TCAs, Melatonin & Meperidine— Serotonin Syndrome
6- MAO-1 -Enzyme inhibitors— Potentiate other drugs e.g. Alcohol.
19
Q
Treatment of cheese reaction caused by MAO inhibitors
A
Treatment by IV Phentolamine or Nitroprusside +B-Blocker.
20
Q
Therapeutic Uses: mood stabilizer for:
A
1- Prophylaxis of Manic-Depressive disorder.
2- Prophylaxis of recurrent endogenous depression.
3- Acute mania but slow onset. So, add antipsychotic drug as haloperidol
4- Management of aggressive & violent behavior in prisoners.
21
Q
Hallucinogens,
A
1- Lysergic Acid Di-Ethylamide
2- Mescaline
3- Khat
4- Phencyclidine
4- Psilocybin
5- Ketamine
6- Salvia divinorum
7- Gamma-hydroxybutyric acid
22
Q
Dynamics of L-DOPA:
A
1- L-DOPA (Prodrug) by Central Dopa Decarboxylase (CDD)—Dopamine—{ D2-
receptors
2- Best results are obtained in the first few (3-4) years (loss of dopaminergic
nigrostriatal nerve terminals occurs later)
3- Treats all manifestations of Parkinsonism, especially Bradykinesia>Tremors by
stimulating D2 receptors in basal ganglia.
23
Q
MAO b inhibitor
A
selegilline
24
Q
Desirable = Favorable: increase L-DOPA effect
A
1- Peripheral Dopa Decarboxylase Inhibitor as carpidopa( sinemet) and bsenserazide (Madropar
2- MAO-B inhibitor e.g. Selegiline
3- COMT-Inhibitors e.g. Tolcapone&Entacapone.
4- Anti-Muscarinic drugs e.g. Benztropine.
25
Undesirable = Unfavorable: decrease Ldopa
- Dopamine (o2 receptor blockers:
a- Neuroleptics e.g. Phenothiazines & Butyrophenones.
b- Anti-emetics e.g. Metoclopramide.
2- Pyridoxine (Vit Bs)—r PDD—Accelerates peripheral decarboxylation — Dopamine.
B- With Non-selective MAQ-l— Severe hypertension.
26
Contraindications of Direct Dopamine Agonist
Psychotic illness
Active peptic ulcer
Peripheral Vascular Diseases
26
Adverse effects of direct dopamine agonists:
a- GIT: Anorexia and nausea and vomiting which can be minimized by taking the
medication with meals. Constipation, dyspepsia & Bleeding from peptic ulceration.
b- CVS:
Postural hypotension may occur, particularly at the initiation of therapy.
Painless digital vasospasm is a dose-related complication of long-term
treatment with the ergot derivatives (bromocriptine or pergolide).
o Cardiac arrhythmias occur (an indication for discontinuing treatment).
Cardiac valvulopathy may occur with pergolide.
c CNS Dyskinesia
d- Mental disturbances.
e- Erythromyalgia (swollen, red, hot & tender feet).
27
latrogenic Parkinsonism = Drugs Contra-indicated in parkinsonism
1- Blockers of Central D,-receptors:
a- Neuroleptic drugs: Phenothiazines & Butyrophenones.
b- Antiemetics: Metoclopramide.
2- Reserpine — Depletion of Dopamine stores
3- Alpha-methyl Dopa — Inhibition of Dopamine synthesis
4- Destruction of Dopamine neurons: MPTP.
5- Parasympathomimetic drugs that pass BBB: Physostigmine & Pilocarpine.
28
Adverse Effects of Phenytoin:
1- CNS:— Confusion & Hallucinations. Ataxia, Nystagmus & Vertigo (dose-dependent)
2- GIT: Gastric irritation (highly alkaline) —anorexia, nausea, vomiting— Used after
meals.
3- Blood: megaloblastic anemia, hypoprothrombinemia
4- Bone: osteomalacia
5- Hirsutism (Androgenic effect).
6- Hepatotoxicity.
7- Hypersensitivity - Lymphadenopathy (Misdiagnosed for Hodgkin’s disease) & Lupus.
8- Hormones — { Release of A.D.H. & Insulin Hyperglycemia.
9- Gum (Gingival) Hyperplasia especially in Children — Irreversible — Consult Dentists.
10- During Pregnancy:
a- First trimester — Teratogenic — Fetal Hydantoin Syndrome — Hare lip & Cleft palate
29
Carbamazepine MoA
It blocks sodium channels, thereby inhibiting the generation of repetitive action potentials in the epileptic focus and preventing their spread
-Related to Tri-cyclic Anti-depressants — Useful as Mood Stabilizer in patients with Manic-Depressive Disorders.
30
causes steven johnson syndrome
carbamazepine
lamotrigine
31
# written
Adverse Effects of carbazepine
a- CNS: Ataxia, Nystagmus & Vertigo — Cerebello-Vestibular
b- GIT: Anorexia, nausea, vomiting — G.I.T. upset
¢-Blood: Bone marrow inhibition—leukopenia, agranulocytosis
d- Anti-diuretic — Fluid retention, hyponatremia
e- Hepatitis
f- Teratogenic — Similar to Fetal Hydantoin Syndrome.
g- Allergy, Stevens-Johnson syndrome
32
# written
Mechanism of Antiepileptic Action of Valproic Acid & Sodium Valproate
a- Block Na*-channels— Similar to Phenytoin. Effective in Partial &Grand Mal epilepsy.
b- Block T-Ca-Channels— Similar to Ethosuximide — Effective in Absence seizures.
c- {_GABA-transaminase enzyme —»{t GABA (membrane hyperpolarization)
d- Antagonize excitatory transmitters e.g. Aspartat
33
# w
Therapeutic use of valproic acid & sodium valproate
a- Broad Spectrum Anti-epileptic useful in Grand mal epilepsy, Partial seizures& Petit
mal epilepsy (Not drug of choice — Sedation & Hepatotoxic).
b- Drug of choice in patients with:
- Mixed Petit mal + Grand mal epilepsy.
- Myoclonic epilepsy.
c- Other Uses:
a- Mood stabilizer in manic depressive disorders.
b- Migraine headache
34
# w
Adverse Effects of Valproic acid
a- C.N.S. - Sedation
b- G.L.T. - Nausea & Vomiting.
c-Blood — Thrombocytopenia & ¢ Platelet aggregation - Hemorrhage.
d- Hepatotoxicity.
e- Temporary loss of hair — Thin curly hair
f- Teratogenic — neural tube defect (Spina bifida).
g- Allergy
35
Therapeutic Uses of Morphine
1- Pain: Analgesic in Severe Visceral Pain
a- Cardiac pain e.g. Myocardial infarction
b- Cancer pain especially in terminal stages
¢- Colic: Add Atropine in Biliary & Renal colic.
d- Bone Fractures (Except Skull, Morphine is contraindicated in Head injury).
e- Postoperative: Except Biliary & Eye operations.
2- Pulmonary Edema due to Acute Left Ventricular Failure:
3 -Primary Neurogenic shock
4-Preanesthetic medication:
36
used in Neurolept-Anesthesia
Fentanyl + Droperidol + Nitrous oxide
37
action of salicylates on blood
- In inflammation, Aspirin — Decrease Elevated Erythrocytic Sedimentation Rate &
Decrease Leukocytosis to normal (No leucopenia).
- Hypoprothrombinemia: Aspirin Large Dose for long time — warfarin like - Compete
with Vit-K in liver - Decrease Synthesis of activated Prothrombin & factors VII, IX & X.
- Decrease_Platelet Aggregation: Aspirin Small dose (75 — 150 mg) — Irreversible
inhibition of thromboxane Az (TXA2) synthesis.
- Hemolysis(Idiosyncrasy)in patients with (G6PD deficiency) as Favism.
38
# w
Therapeutic Uses of Salicylates:
A) Local Uses:
1- Salicylic acid:
a- Keratolytic in coms & warts (Salicylic acid 20% in collodion).
b- Fungistatic in Tinea of Skin (Salicylic acid + Benzoic acid).
c- Antiseptic in Hyperhidrosis (Salicylic acid + Talcum powder).
2- Methyl-Salicylate (Oil of Wintergreen) — Counter-irritant in Arthritis & Myositis.
B) Systemic Uses:
(Uses 1. 2 & 3: Dose 1 - 2 g/day in divided doses,
Uses 4. 5 & 6: Dose 6 g/ day in divided doses)
1- Anti-pyretic— Non-specific & Non-causal.
2- Analgesic in Mild superficial pains e.g. Headache, toothache, myalgia, arthralgia &
Neuralgia. Effective in dysmenorrhea (PG) but may Increase Bleeding.
3- Common cold— Treat Fever, headache, muscle and joint pains.
4- Rheumatic fever (Arthritis) — Treat fever, arthritis, decreases ESR, decreases
Leukocytosis. NOT effective in Carditis, Chorea or Cutaneous nodules.
5- Rheumatoid arthritis
6- Chronic gout (Alkalinize urine & increase Fluid intake).
7- Antiplatelet (75-150 mg/day) — Prophylaxis against thromboembolic diseases.
39
# w
Adverse Effects & Toxicity of Salicylates:
2- Salicylism: Large dose for Long time — Tinnitus, blurring of vision, GIT upset,
irritability & hyperventilation. Reversible after stopping salicylates.
3- Hypoprothrombinemia — Bleeding tendency.
4- G.1.T. irritation — Nausea, voting, pain, ulceration & bleeding (Misoprostol is a PGE1
analog useful in treatment of NSAID-induced peptic ulcer).
5- Allergy (Hypersensitivity) — Rash, urticaria, angioedema & Bronchial asthma.
*Bronchial asthma may be Ag/Ab reaction or inhibit COX — Shift to LOX —increases
LT. LOX-inhibitors (Zileuton) & Cysteinyl LT-1 receptor blocker (Montelukast) are
useful in Aspirin-induced asthma
6- Reye’s syndrome: Aspirin in some children with viral infection (e.g. Influenza or
Chicken pox) — Encephalopathy & Hepatotoxicity.
7- Teratogenicity — Cardiac septal defect.
8- |diosyncrasy — Hemolysis in patients with Favism.
9- Nephropathy.
40
Pyrazolone Derivatives
Azapropazone: uricosuric
41
Indole Derivatives and uses
Indomethacin
Very Potent Antipyretic analgesic & Anti-Rheumatic
Uses:
- closure of patent ductus arteriosus.
- Acute gouty arthritis
42
uses of diclofenac
a- Inflammations e.g. Arthritis, Myositis & Acute Gout.
b- Colic e.g. Dysmenorrhea.
c- Eye drops to treat ocular inflammations e.g. Postoperative.
43
Selective COX-ll Inhibitors uses
It is used for the short-term treatment of postoperative
pain. It is given by intravenous or intramuscular injection.
44
# w
Dynamics of Paracetamol
1- Inhibit COX-3 in C.N.S.Mainly— Anti-pyretic Analgesic — As potent as Aspirin.
2- Aimost No peripheral Action — Almost No Anti-inflammatory & Aimost No effect on
respiration, C.V.S., Platelet aggregation, Gastric acidity or Uric acid.
45
# w
Therapeutic uses of Paracetamol
** Antipyretic Analgesic **(1/2 - 1 g) especially in patients who cannot
tolerate aspirin e.g. Allergy to Aspirin, Bronchial asthma, Children with viral infection,
Bleeding tendency, Peptic ulcer & Gout.
46
# w
Adverse Effects & Toxicity of parcetamol
1-Toxic dose of Paracetamol (> 10 g in Adults & 4 g in Children) — Depletion of
Glutathione-SH —>Hepatotoxic & Nephrotoxic— Fatal.
Management: |.V. N-Acetylcysteine (Rich in S-H) + Oral Methionine.
2- Allergy (Hypersensitivity).
47
Actions of colchicine
A) Anti-Gout Effect:
1-Effective in treatment of Acute Attack of Gout.
2- NOT effective in other types of arthritis.
3- NOT affect uric acid synthesis or excretion or blood level.
4- 1t binds to Microtubular protein (Tubulin) of polymorph nuclear leucocytes
(P.M.N.L) -8 Migration of P.M.N.L. to joints -NO Phagocytosis of Mono-sodium
urate crystals —-NO Ruptures of leukocytes —NO release of lactic acid -NO
Inflammatory acidity — NO further precipitation &NO release of chemotactic factors
e.g. Glycoproteins, IL-1 or LTB4 of urate crystals
B) Anti-Mitotic Effect—Inhibits cell division.
At higher doses than are used to treat gout, colchicine inhibits mitosis, carrying a
risk of serious bone marrow depression.
48
Therapeutic Uses of colchicine
1- Acute attacks of gout
2- Prophylaxis of Gout:
3- Prophylaxis of Familial Mediterranean Fever (Polyserositis).
49
Adverse Effects of colchicine
1- G.L.T.— Nausea, vomiting &Diarrhea.
2- Hepatotoxicity
3- Nephrotoxicity —» Hematuria & Oliguria.
4- Bone marrow depression
5- Myopathy.
6- Reversible alopecia.
50
Actions Xanthine-Oxidase Inhibitors- Allopurinol
1- Allopurinol is metabolized by Xanthine Oxidase enzyme(XOE) — Alloxanthine
2- Both Allopurinol & Alloxanthine — Occupy & inhibits X.0.E. — deceases Synthesis of uric acid.
3- It has NO effect on renal excretion of uric acid.
50
Therapeutic Uses of allopurinol
first line therapy for treatment of Hyperuricemia & Chronic
Gout between attacks especially in:
a- Gouty nephropathy & urate renal stones.
b- Associated with the use of Anti-Cancer drugs.
¢- If uricosuric drugs are ineffective or contraindicated.
51
first line therapy for treatment of Hyperuricemia & Chronic Gout
Adverse Effects
a-Precipitates acute attacks of gout during initiation of treatment ( (possibly as a
result of physicochemical changes in the surfaces of urate crystals as they start to redissolve and also due to sudden lowering of serum urate)— Add Colchicine or NSAID
prophylactically.
b- C.N.S. - Headache & psychological changes.
¢- Allergic skin reaction (mainly rash)
d- G.I.T. disturbances.
e- Hepatomegaly.
f- Leucopenia.
g- Better avoided in children & during lactation (safety not yet established).
h- Drug Interaction:
o & Metabolism of Probenecid & Mercaptopurine (which is inactivated by xanthine
oxidase) — Toxicity.
The effect of warfarin is increased because its metabolism is inhibited
51
As with allopurinol, prophylactic treatment with colchicine or NSAID should be started
at the beginning of therapy to avoid gout flares
Febuxostat
52
More selective and potent inhibitor of xanthine oxidase than allopurinol.
Febuxostat
53
Therapeutic Uses Of aminophylline
1- Bronchial Asthma: acute attacks and status athmaticus
2- Chronic Obstructive Pulmonary Diseases emhysema
3- Cardiac Asthma
53
CNS stimulants
Analeptic stimulants:
Psychomotor stimulants:
Methylxanthines:
Psychotomimetic stimulants (hallucinogenic drugs).
54
Caffeine uses
1- With Ergotamine — Cafergot in acute attack of Migraine headache.
With Aspirin or paracetamol in simple headache.
2- Fatigue (Physical or mental).
3- With Neostigmine in Myasthenia Gravis.
4- Overdose of C.N.S. depressants e.g. Hypnotics.
55
methylxanthine derivative used in treatment of:
- Chronic occlusive arterial diseases e.g. intermittent claudication:
Pentoxifylline
56
# w
Anti-Bacterial Activity: of b lactams antibiotics
1- Bactericidal Antibiotics.
2- They bind to specific_Penicillin-Binding-Protein (PBP), at least 7 types:
a- inhibit Transpeptidase enzyme responsible for cross-linking of peptidoglycans, a final step in cell wall synthesis —{ Cell Wall Synthesis.
b- Activate Autolytic enzymes (Autolysins) — Lysis of cell wall.
c- Bacteria imbibe water due to its interior high osmotic pressure — Rupture and DEATH of the microbe.
d- They affect mainly growing bacteria rather than resting one.
3- Selectivity: Human cells do not contain peptidoglycan cell wall.
4- Resistance:
a- Natural absence of peptidoglycan cell wall e.g. Mycoplasma.
b- Acquired resistance:
o Production of B-lactamase enzymes (Too many types).
Some of them are specific penicillinases & cephalosporinases.
57
Sulbactam + Ampicillin
Unasyn
58
Tazobactam + Piperacillin
Tazocin
59
59
60
61
62
# w
Antibiotic associated (Pseudomembranous) colitis. Caused by enterotoxins produced by Staph. or Clostridium difficil. Treated by
Oral Vancomyein or
Metronidazole.
63
prophylactic uses of penicillin
1. streptococcal infection in rhematic fever
2. bacterial endocarditis
3. gonorrheal neonatal ophtalmia
64
against gram positive organisms and gram negativ bacilli including E.coli and klebsiellla pneumonia, but not H. influenza , proteus , P. aeruginosa
first generation cephalosporins
65
bacteria spectrum of second generation cephalosporins
less active against gram positive
more active against gram negative h influenza
66
fourth generation cephalosporins
cefepime
67
oganism resistant to tigecycline
P.aeruginosa
68
