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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
B blockers with local anesthetic effect
Acebutol Labetalol Metoprolol Pindolol Propranolol
26
Spasmolytic agents
Diazepam: GABA-A agonist Baclofen: GABA-B agonist Tizanidine: a2 agonist Tolperisone: Inhibition of Ca2+ and Na+ ch.
27
Diazepam receptror preferance
GABA-A DiAAAAAzepam
28
Diazepam MOA
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
29
Diazepam metabolism and duration of action
Hepatic | 12-24 h
30
Diazepam indications
Centrally-acting spasmolytlcs - Chronic spasm (Cerebral palsy, stroke, spinal injury) - Acute spasm due to muscle injury
31
Diazepam side effects
CNS depressant Tolerance Dependent liability
32
What is an GABA-B agonist?
Baclofen
33
Baclofen MOA
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
34
Baclofen | How to give?
Oral | Intrathecal for severe spasticity
35
Baclofen indications
Spasm (Cerebral palsy, stroke, multiple sclerosis)
36
Baclofen side effects
Sedation Weakness Rebound spasticity when abrupt withdrawal
37
Spasmolytic a2 agonist
Tizanidine
38
Tizanidine | Tell me about it
- 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
39
Tizanidine indications
Spasm (stroke, multiple sclerosis) -Oral for acute and chronic spasms
40
Tizanidine side effects
``` Wekness Sedation Hypotension Hepatotoxiciy Rebound HTN when abrupt withdrawal ```
41
Tolperisone MOA
Inhibition of muscle stretch reflex Reduction of muscle reflex Oral Hungarian -inhibition of Na & Ca channels
42
Tolperisone indication
Acute spasm due to muscle injury | No used in chronic spasm
43
Tolperisone side effects
Sedation Confusion Ocular effects Strong anti muscarinic effects SOS-C
44
Direct acting muscle relaxants
Dantrolene | Botulinium toxin
45
Dentrolene MOA
RyR1 antagonist → Blocks Ca2+ release ch. in the Sarcoplamis reticulum of skeletal muscle → reduces actin-myosin interaction
46
Dentrolene | How to give? Duration?
Oral, IV | 4-6 h
47
Dentrolene indications
- Malignant hyperthermia (IV) - Neuroleptic malignant syndrome (NMS) Spasm (Crebral palsy, multiple sclerosis) -Oral for acute and chronic spasms
48
Dentrolene side effects
Muscle weakness | Hepatotoxicity
49
Botulinium toxin MOA
Prevent synaptic exocytosis through inhibition of SNARE fusion proteins in presynaptic nerve terminals → Flaccid paralysis
50
Botulinium toxin | How to give? Duration?
Direct IM | 2-3 months
51
Botulinium toxin indications
-Upper and lower limb spasm (Crebral palsy, multiple sclerosis) - Cervical dystonia - Migrane - Overactive bladder - Hyperhidrosis Cosmetics
52
Non depolarizing neuromascular blocking agents
Cisatra-curium Miva-curium Ro-curonium Pan-curonium
53
Non depolarizing neuromascular blocking agents duration of action
-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
``` Atracuriun Cisatracurium Mivacurium Rocuronium Pancuronium ``` Which is a steroid?
Rocuronium ( Hepatic) Pancuronium (Renal, unchanged in urine)
55
``` Atracuriun Cisatracurium Mivacurium Rocuronium Pancoronium ``` Metabolism
- Cisatracurium: Spontaneous breakdown (Hofmann elimination) less laudonosine - atracurium: Spontaneous breakdown (Hofmann elimination) - Mivacurium: Pseudocholinesterase - Rocuronium: Hepatic - Pipecoronium: Renal
56
Atracurium cisatracurium Mivacurium side effects
- Histamine release (Hyotension) - Prolonged apnea (Muscle weakness) Laudanosine formation (atracurium) --> provoke seizure in renal impairement
57
Cisatracurium side effects
``` Histamine release (Hyotension) Prolonged apnea (Muscle weakness) ```
58
Mivacurium SE
``` Histamine release (Hyotension) Prolonged apnea (Muscle weakness) ``` -withdrawn from market in USA
59
Rocuronium SE
Prolonged apnea (Muscle weakness)
60
Most potent neuromascular blocking agent
Pipecuronium
61
Depolarizing neuromascular blocking agents
Succinylcholine (Suxamethonium)
62
Succinylcholine | How to give? Duration of action? metabolism?
Parenteral 5 min Rapid metabolism by plasma cholinesterase
63
Succinylcholine indications
Intubation Endoscopy ECT "electro-convulsive therapy)
64
Succinylcholine side effects
Arrhthmias Hyperkalemia Postoperative muscle pain Malignant hyperthermia
65
B agonists
Sabutamol (Albuterol) Terbutaline Feno.terol Salme.terol Formo.terol
66
Long acting B2 agonists
Salmeterol Formoterol they Flow Slow More Formal We are Salmates
67
Short acting B2 agonists
Salbutamol Terbutaline Fenoterol Fest, Salbation, Terter
68
SABA Duration of action Onset of action How to give?
< 4 h 5 min Aerosol, nebulizer, parenteral
69
LABA Duration of action How to give?
12-14 h | Aerosol, nebulizer, parenteral
70
Short acting B2 agonists indications
Asthma COPD Acute asthmatic bronchospasm Not effective in asthma prophylaxis
71
B2 agonists side effects
Tachycardia Tremor Arrhythmia
72
Which B2 agonist is used to suppress premature labor
Terbutaline
73
LABA indications
Bronchodilation in asthma and COPD Prophylaxis Not effective for acute episodes Combination with corticosteroides is good
74
Muscarinic antagonist used in asthma | Which is longer acting?
Tiotropium is longer acting than Ipratropium
75
Methylxantine used in asthma?
Theophylline (tea)
76
Theophylline How to give Duration of action
Oral | Slow onset, 12 h diration of action
77
Theophylline metabolism
CYP450
78
Theophylline MOA
PDE inhibition → cAMP↑ → Bronchodilation and reduced inflammation Also Adenosine antagonist → CNS effects methylxanthine used in asthma
79
Corticosteroides for the treatment of asthma?
Budesonide beclomethasone Dexamethasone fluticasone Prednisone (oral) Prednisolone (I.V GC) methylprednisolone ( oral, parenteral)
80
Budesonide Dexamethasone Duration of action
10-12 h
81
Prednisone Duration of action
12-24 h
82
Budesonide Dexamethasone Prednisone Which is oral and which is inhaled?
Budesonide: inhaled Dexamethasone: inhaled Prednisone: oral
83
Methylprednisolone is given how?
Oral | IM, SC
84
Methylprednisolone duration of action
12-36 h
85
Prednisone side effects
Systemic toxicity appear when systemic treatment > 2 weeks ``` Adrenal suppression, growth inhibition, muscle wasting, osteoporosis, salt retention, glucose intolerance, behavioral changes ```
86
Budesonide side effects
Oropharyngeal candidiasis
87
Leukotriens antagonist
Monteleukast
88
Monteleukast MOA
LTD4-R antagonist - reduce inflammation - decrease bronchoconstriction
89
Monteleukast | How to give? Duration of action?
Oral | 12-24 h
90
Monteleukast indications
Asthma prophylaxis Oral treatment in children Minimal side effects!
91
Selective inhibitor of LOX enzyme
Zileuton
92
Anti IgE Ab
Omalizumab
93
Omalizumab molecule properties
human monoclonal IgG Ab against Fc region of IgE
94
Omalizumab How to give? Indications?
Parenteral | Prophylaxis for severe asthma that is not responsive for other drugs
95
What can we give topically for rhinitis?
Fluticasone
96
Which drug desensitize the stretch receptors in the lungs?
Prenoxdiazine
97
Prenoxdiazine | Whaat is special about it?
peripherally acting anti-tussive ( like lidocaine) | Does not cause addiction
98
Prenoxdiazine indications
Cough from bronchial origin
99
Codeine What is it? Duration? Indications?
Opioid derivative Short duration Acute and chronic dry cough
100
Codeine MOA
Mue receptor agonist- Suppress cough reflex
101
Non opioid centrally acting antitussives
Butamirate pentoxyverine
102
Butamirate indications
Cough | COPD (maybe)
103
Muco-active drugs
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
Acetylcysteine MOA | How to give?
Reduces disulfide bonds in mucus matrix → Mucus viscosity ↓ Oral mucolytic
105
Bromhexine MOA
Increase the production of serous fluid in the respiratory tract whcih maces mucus thinner and less viscous
106
Mucoactive agents: Acetylcysteine Bromhexine Indications
CF Chronic bronchitis Bronchiectasis
107
General treatment- Peripheral Vascular Disease
``` Life style modification Glycemic control Dyslipidemia control with Statins Anti PLT therapy with Aspirin or Clopidorgrel BP control ACE/ARB's ```
108
Specific treatment- Peripheral Vascular Disease | 5 drugs
``` Cilostazol Pentoxifylline Vinpocetine Nicergoline Calcium dobesilate ```
109
Cilostazol MOA | How to give
PDE-3 inhibitor → PLT aggregation ↓, Vasodilation, LPL activity ↑ Oral
110
Cilostazol indications and side effects
Intermittent caludication Headache, palpitations, vertigo, coronary steal synd.
111
Cilostazol contraindication
CHF congestive heart failure because of evidence of reduced survival.
112
Intermittent caludication
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
Pentoxifylline MOA
Reducing the viscosity of blood and increases deformability of RBC → Blood flows more easily through obstructed vessel competitive nonselective PDE-inhibtior rheological agent
114
Pentoxifylline indications
Atherosclerosis circulatory disease Diabetic circulatory disease Intermittent caludication
115
Pentoxifylline side effects
``` GI Tachycardia Angina Cutaneous flushing Allergy ```
116
Migrane specific treatment
Sumatriptan
117
Sumatriptan MOA
Selective 5-HT1D/1B agonist
118
Sumatriptan indications
Acute migrane attack
119
Sumatriptan side effects
Abnormal sensation Dizziness Chest pain Coronary vasospasm
120
Migrane prophylaxis therapy drugs (7)
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
When do we give Migrane prophylaxis therapy?
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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