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pharmacology final ( 1st sem) > B: 8-13 > Flashcards

B: 8-13 Flashcards

1
Q

Non selective B-R antagonists

A

Propranolol
Timolol
Pindolol
Sotalol

Pls Tell People Sorry- we dont treat CHF

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2
Q

Which Non selective B-R antagonists is given topically?

To treat what?

A

Timolol

Glaucoma

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3
Q

Propranolol drug properties

A 
Oral, Parenteral
Higly lipid solubule
Freely enters CNS
4-6 h
Local anesthetic effect
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4
Q

Which Non selective B-R antagonists has a local anesthetic effect and how?

A

Propranolol

Bcs. it inhibits Na+ ch.

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5
Q

Propranolol indications

A 
HTN
Antiarrhytmic class II (treat + prophylaxis)

Thyrotoxicosis
Essential tremor
Angina
Migraine

HA - TEAM

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6
Q

How does Propranolol treat angina?

A

↓ HR
↓ O2 demand

↑ diastolic perfusion

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7
Q

Pindolol effect

A

partial agonist action; less bronchospasm for pts with asthma
Intrinsic sympathoimetic activity
Local anesthetic effect

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8
Q

Pindolol indications

A

Hypertensive treatment in asthma/COPD patients

Avoid in HF!

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9
Q

Which Non selective B-R antagonists should be avoided in HF?

A

Pindolol

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10
Q

Sotalol R preferance

A

B non selective

K+ ch. antagonist

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11
Q

Sotalol

How to give? Duration of action?

A

Oral

7 h

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12
Q

Sotalol indications

A

Antyarrhythmic class III
Ventricular arrhythmias
A. Fib

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13
Q

Sotalol side effects

A

Dose dependent Torsade-de-Pointes

אתה שותה סודה וזה מוריד ומרים אותך כמו טידיפי באקג

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14
Q

B1 selective antagonists

A

A-BEAM

Atenolol
Bisoprolol
Esmolol
Acebutalol- partia agonis
Metoprolol

Nevibolol

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15
Q

Metoprolol
Bisoprolol
Nebivolol

Indications

A 
HTN
Chronic HF
Angina
AA class II
Acute coronary syndrome

HC-AAA

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16
Q

Which B blocker has an NO dependant vasodil. effect?

A

Nebivolol

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17
Q

Metoprolol
Bisoprolol
Nebivolol

Which has the longest duration of action?

A

Bisoprolol

עושה להם בית ספר

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18
Q

Which B blocker has a local anesthetic effect?

A

B1-selective:
Metoprolol
Acebutol

non-selective:
Pindolol
Propanolol

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19
Q

Which B blocker has a short (10 min) duration of action?

A

Esmolol (IV)

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20
Q

Esmolol indications

A

Arrhythmias assosiated with thyroid storm
Perioperative
Hypertensive emergencies

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21
Q

B blockers side effects

A 
AV block
Heart failure
Bradyarrhythmias
Bronchospasms (fatal in asthmatics)
CNS seadtion
Hypoglycemia
Hyperlipidemia
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22
Q

Highest lipid solubility B blockers

A

Propranolol
Nebivolol
Bisoprolol

Peanut butter N jelly it has a lot of fat

BPN

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23
Q

lowest lipid solubility B blockers

A

Atenolol
Sotalol

If you want nice ass you need to eat less fat

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24
Q

B blockers contraindications

A

Acute heart failure
Cardiogenic shcok
Careful in case of Asthma/COPD
Careful in DM

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25
Q

B blockers with local anesthetic effect

A

Acebutol
Labetalol
Metoprolol

Pindolol
Propranolol

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26
Q

Spasmolytic agents

A

Diazepam: GABA-A agonist
Baclofen: GABA-B agonist
Tizanidine: a2 agonist
Tolperisone: Inhibition of Ca2+ and Na+ ch.

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27
Q

Diazepam receptror preferance

A

GABA-A

DiAAAAAzepam

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28
Q

Diazepam MOA

A

Increases interneuron inhibition of primary motor afferents in spinal cord

  • bind post synaptic GABA-A receptor –> facilitate Cl- channel opening and increase frequency
  • membrane hyperpolarization
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29
Q

Diazepam metabolism and duration of action

A

Hepatic

12-24 h

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30
Q

Diazepam indications

A

Centrally-acting spasmolytlcs

  • Chronic spasm (Cerebral palsy, stroke, spinal injury)
  • Acute spasm due to muscle injury
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31
Q

Diazepam side effects

A

CNS depressant
Tolerance
Dependent liability

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32
Q

What is an GABA-B agonist?

A

Baclofen

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33
Q

Baclofen MOA

A

Pre and post synaptic inhib. of motor output in the spinal cord

Pre- and postsynaptic
GABA-B receptor activation –> facilitate spinal inhibition of motor neurons

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34
Q

Baclofen

How to give?

A

Oral

Intrathecal for severe spasticity

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35
Q

Baclofen indications

A

Spasm (Cerebral palsy, stroke, multiple sclerosis)

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36
Q

Baclofen side effects

A

Sedation
Weakness
Rebound spasticity when abrupt withdrawal

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37
Q

Spasmolytic a2 agonist

A

Tizanidine

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38
Q

Tizanidine

Tell me about it

A
  • a2 Agonist in spinal cord
  • Pre and post synaptic inhibition of reflex motor output in the spinal cord

Oral
Renal and hepatic elimination
3-6 h

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39
Q

Tizanidine indications

A

Spasm (stroke, multiple sclerosis)

-Oral for acute and
chronic spasms

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40
Q

Tizanidine side effects

A 
Wekness
Sedation
Hypotension
Hepatotoxiciy
Rebound HTN when abrupt withdrawal
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41
Q

Tolperisone MOA

A

Inhibition of muscle stretch reflex
Reduction of muscle reflex
Oral
Hungarian

-inhibition of Na & Ca channels

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42
Q

Tolperisone indication

A

Acute spasm due to muscle injury

No used in chronic spasm

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43
Q

Tolperisone side effects

A

Sedation
Confusion
Ocular effects
Strong anti muscarinic effects

SOS-C

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44
Q

Direct acting muscle relaxants

A

Dantrolene

Botulinium toxin

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45
Q

Dentrolene MOA

A

RyR1 antagonist → Blocks Ca2+ release ch. in the Sarcoplamis reticulum of skeletal muscle → reduces actin-myosin interaction

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46
Q

Dentrolene

How to give? Duration?

A

Oral, IV

4-6 h

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47
Q

Dentrolene indications

A
  • Malignant hyperthermia (IV)
  • Neuroleptic malignant syndrome (NMS)

Spasm (Crebral palsy, multiple sclerosis)

-Oral for acute and chronic
spasms

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48
Q

Dentrolene side effects

A

Muscle weakness

Hepatotoxicity

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49
Q

Botulinium toxin MOA

A

Prevent synaptic exocytosis through inhibition of SNARE fusion proteins in presynaptic nerve terminals → Flaccid paralysis

50
Q

Botulinium toxin

How to give? Duration?

A

Direct IM

2-3 months

51
Q

Botulinium toxin indications

A

-Upper and lower limb spasm (Crebral palsy, multiple sclerosis)

  • Cervical dystonia
  • Migrane
  • Overactive bladder
  • Hyperhidrosis

Cosmetics

52
Q

Non depolarizing neuromascular blocking agents

A

Cisatra-curium
Miva-curium
Ro-curonium
Pan-curonium

53
Q

Non depolarizing neuromascular blocking agents duration of action

A

-Mivacurium: 10-15 min

Atracurium ( toxic metabolite laudonosine provokes seizures in renal impairment)
Cisatracurium: 20-30 min ( metabolism INDEPENDENT on hepatic, renal function)

  • Rocuronium: 20-30 min
  • Pipecoronium: 60-180 min
54
Q 
Atracuriun
Cisatracurium
Mivacurium
Rocuronium
Pancuronium

Which is a steroid?

A

Rocuronium ( Hepatic)

Pancuronium (Renal, unchanged in urine)

55
Q 
Atracuriun
Cisatracurium
Mivacurium
Rocuronium
Pancoronium

Metabolism

A
  • Cisatracurium: Spontaneous breakdown (Hofmann elimination) less laudonosine
  • atracurium: Spontaneous breakdown (Hofmann elimination)
  • Mivacurium: Pseudocholinesterase
  • Rocuronium: Hepatic
  • Pipecoronium: Renal
56
Q

Atracurium
cisatracurium
Mivacurium
side effects

A
  • Histamine release (Hyotension)
  • Prolonged apnea (Muscle weakness)

Laudanosine formation
(atracurium) –> provoke seizure in renal impairement

57
Q

Cisatracurium side effects

A 
Histamine release (Hyotension)
Prolonged apnea (Muscle weakness)
58
Q

Mivacurium SE

A 
Histamine release (Hyotension)
Prolonged apnea (Muscle weakness)

-withdrawn from market in USA

59
Q

Rocuronium SE

A

Prolonged apnea (Muscle weakness)

60
Q

Most potent neuromascular blocking agent

A

Pipecuronium

61
Q

Depolarizing neuromascular blocking agents

A

Succinylcholine (Suxamethonium)

62
Q

Succinylcholine

How to give? Duration of action? metabolism?

A

Parenteral
5 min
Rapid metabolism by plasma cholinesterase

63
Q

Succinylcholine indications

A

Intubation
Endoscopy
ECT “electro-convulsive therapy)

64
Q

Succinylcholine side effects

A

Arrhthmias
Hyperkalemia
Postoperative muscle pain
Malignant hyperthermia

65
Q

B agonists

A

Sabutamol (Albuterol)
Terbutaline
Feno.terol

Salme.terol
Formo.terol

66
Q

Long acting B2 agonists

A

Salmeterol
Formoterol

they Flow Slow
More Formal
We are Salmates

67
Q

Short acting B2 agonists

A

Salbutamol
Terbutaline
Fenoterol

Fest, Salbation, Terter

68
Q

SABA
Duration of action
Onset of action
How to give?

A

< 4 h
5 min
Aerosol, nebulizer, parenteral

69
Q

LABA
Duration of action
How to give?

A

12-14 h

Aerosol, nebulizer, parenteral

70
Q

Short acting B2 agonists indications

A

Asthma
COPD
Acute asthmatic bronchospasm
Not effective in asthma prophylaxis

71
Q

B2 agonists side effects

A

Tachycardia
Tremor
Arrhythmia

72
Q

Which B2 agonist is used to suppress premature labor

A

Terbutaline

73
Q

LABA indications

A

Bronchodilation in asthma and COPD
Prophylaxis
Not effective for acute episodes
Combination with corticosteroides is good

74
Q

Muscarinic antagonist used in asthma

Which is longer acting?

A

Tiotropium is longer acting than Ipratropium

75
Q

Methylxantine used in asthma?

A

Theophylline (tea)

76
Q

Theophylline
How to give
Duration of action

A

Oral

Slow onset, 12 h diration of action

77
Q

Theophylline metabolism

A

CYP450

78
Q

Theophylline MOA

A

PDE inhibition → cAMP↑ → Bronchodilation and reduced inflammation

Also Adenosine antagonist → CNS effects

methylxanthine used in asthma

79
Q

Corticosteroides for the treatment of asthma?

A

Budesonide
beclomethasone
Dexamethasone
fluticasone

Prednisone (oral)
Prednisolone (I.V GC)

methylprednisolone ( oral, parenteral)

80
Q

Budesonide
Dexamethasone

Duration of action

A

10-12 h

81
Q

Prednisone

Duration of action

A

12-24 h

82
Q

Budesonide
Dexamethasone
Prednisone

Which is oral and which is inhaled?

A

Budesonide: inhaled
Dexamethasone: inhaled
Prednisone: oral

83
Q

Methylprednisolone is given how?

A

Oral

IM, SC

84
Q

Methylprednisolone duration of action

A

12-36 h

85
Q

Prednisone side effects

A

Systemic toxicity appear when systemic treatment > 2 weeks

Adrenal suppression,
growth inhibition, 
muscle wasting, 
osteoporosis,
 salt retention,
glucose intolerance,
behavioral changes
86
Q

Budesonide side effects

A

Oropharyngeal candidiasis

87
Q

Leukotriens antagonist

A

Monteleukast

88
Q

Monteleukast MOA

A

LTD4-R antagonist

  • reduce inflammation
  • decrease bronchoconstriction
89
Q

Monteleukast

How to give? Duration of action?

A

Oral

12-24 h

90
Q

Monteleukast indications

A

Asthma prophylaxis
Oral treatment in children
Minimal side effects!

91
Q

Selective inhibitor of LOX enzyme

A

Zileuton

92
Q

Anti IgE Ab

A

Omalizumab

93
Q

Omalizumab molecule properties

A

human monoclonal IgG Ab against Fc region of IgE

94
Q

Omalizumab
How to give?
Indications?

A

Parenteral

Prophylaxis for severe asthma that is not responsive for other drugs

95
Q

What can we give topically for rhinitis?

A

Fluticasone

96
Q

Which drug desensitize the stretch receptors in the lungs?

A

Prenoxdiazine

97
Q

Prenoxdiazine

Whaat is special about it?

A

peripherally acting anti-tussive ( like lidocaine)

Does not cause addiction

98
Q

Prenoxdiazine indications

A

Cough from bronchial origin

99
Q

Codeine
What is it?
Duration?
Indications?

A

Opioid derivative
Short duration
Acute and chronic dry cough

100
Q

Codeine MOA

A

Mue receptor agonist- Suppress cough reflex

101
Q

Non opioid centrally acting antitussives

A

Butamirate

pentoxyverine

102
Q

Butamirate indications

A

Cough

COPD (maybe)

103
Q

Muco-active drugs

A

Acetylcysteine (mucolytic= breaks disulfide bonds in mucus –> decreased viscosity)

Bromhexine (expectorant= increase production of serous fluid –> makes phlegm thinner , less viscous ). (promote sputum excretion)

ambroxol

104
Q

Acetylcysteine MOA

How to give?

A

Reduces disulfide bonds in mucus matrix → Mucus viscosity ↓

Oral

mucolytic

105
Q

Bromhexine MOA

A

Increase the production of serous fluid in the respiratory tract whcih maces mucus thinner and less viscous

106
Q

Mucoactive agents:
Acetylcysteine
Bromhexine

Indications

A

CF
Chronic bronchitis
Bronchiectasis

107
Q

General treatment- Peripheral Vascular Disease

A 
Life style modification
Glycemic control
Dyslipidemia control with Statins
Anti PLT therapy with Aspirin or Clopidorgrel
BP control
ACE/ARB's
108
Q

Specific treatment- Peripheral Vascular Disease

5 drugs

A 
Cilostazol
Pentoxifylline
Vinpocetine
Nicergoline
Calcium dobesilate
109
Q

Cilostazol MOA

How to give

A

PDE-3 inhibitor → PLT aggregation ↓, Vasodilation, LPL activity ↑
Oral

110
Q

Cilostazol indications and side effects

A

Intermittent caludication

Headache, palpitations, vertigo, coronary steal synd.

111
Q

Cilostazol contraindication

A

CHF
congestive
heart failure because of evidence of reduced survival.

112
Q

Intermittent caludication

A

Symptom that describes muscle pain on mild exertion (ache, cramp, numbness or sense of fatigue),[1] classically in the calf muscle, which occurs during exercise, such as walking, and is relieved by a short period of rest. It is classically associated with early-stage peripheral artery disease

113
Q

Pentoxifylline MOA

A

Reducing the viscosity of blood and increases deformability of RBC → Blood flows more easily through obstructed vessel

competitive nonselective PDE-inhibtior

rheological agent

114
Q

Pentoxifylline indications

A

Atherosclerosis circulatory disease
Diabetic circulatory disease
Intermittent caludication

115
Q

Pentoxifylline side effects

A 
GI
Tachycardia
Angina
Cutaneous flushing
Allergy
116
Q

Migrane specific treatment

A

Sumatriptan

117
Q

Sumatriptan MOA

A

Selective 5-HT1D/1B agonist

118
Q

Sumatriptan indications

A

Acute migrane attack

119
Q

Sumatriptan side effects

A

Abnormal sensation
Dizziness
Chest pain
Coronary vasospasm

120
Q

Migrane prophylaxis therapy drugs (7)

A

Galcanezumab (CGRP antagonist)

Cinnarizine (anti-histamine, CCB)

Propranolol (BB)

Verapamil (CCB, non-DiHydroPyridine)

Carbamazepine ( Inhibits VG Na ch, decrease glutamate release)- antiseizure

Valproate (inhibit high freq firing, facilitate inhibitory GABA action- antiseizure

Imipramine (inhibits 5-HT , NE reuptake) TCA

121
Q

When do we give Migrane prophylaxis therapy?

A

Patient presenting with > 4 attacks per month
Attacks are severe and resistance to acute therapy
Prolonged attacks > 72 h

pharmacology final ( 1st sem) (15 decks)

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