B: 8-13 Flashcards
Non selective B-R antagonists
Propranolol
Timolol
Pindolol
Sotalol
Pls Tell People Sorry- we dont treat CHF
Which Non selective B-R antagonists is given topically?
To treat what?
Timolol
Glaucoma
Propranolol drug properties
Oral, Parenteral Higly lipid solubule Freely enters CNS 4-6 h Local anesthetic effect
Which Non selective B-R antagonists has a local anesthetic effect and how?
Propranolol
Bcs. it inhibits Na+ ch.
Propranolol indications
HTN Antiarrhytmic class II (treat + prophylaxis)
Thyrotoxicosis
Essential tremor
Angina
Migraine
HA - TEAM
How does Propranolol treat angina?
↓ HR
↓ O2 demand
↑ diastolic perfusion
Pindolol effect
partial agonist action; less bronchospasm for pts with asthma
Intrinsic sympathoimetic activity
Local anesthetic effect
Pindolol indications
Hypertensive treatment in asthma/COPD patients
Avoid in HF!
Which Non selective B-R antagonists should be avoided in HF?
Pindolol
Sotalol R preferance
B non selective
K+ ch. antagonist
Sotalol
How to give? Duration of action?
Oral
7 h
Sotalol indications
Antyarrhythmic class III
Ventricular arrhythmias
A. Fib
Sotalol side effects
Dose dependent Torsade-de-Pointes
אתה שותה סודה וזה מוריד ומרים אותך כמו טידיפי באקג
B1 selective antagonists
A-BEAM
Atenolol Bisoprolol Esmolol Acebutalol- partia agonis Metoprolol
Nevibolol
Metoprolol
Bisoprolol
Nebivolol
Indications
HTN Chronic HF Angina AA class II Acute coronary syndrome
HC-AAA
Which B blocker has an NO dependant vasodil. effect?
Nebivolol
Metoprolol
Bisoprolol
Nebivolol
Which has the longest duration of action?
Bisoprolol
עושה להם בית ספר
Which B blocker has a local anesthetic effect?
B1-selective:
Metoprolol
Acebutol
non-selective:
Pindolol
Propanolol
Which B blocker has a short (10 min) duration of action?
Esmolol (IV)
Esmolol indications
Arrhythmias assosiated with thyroid storm
Perioperative
Hypertensive emergencies
B blockers side effects
AV block Heart failure Bradyarrhythmias Bronchospasms (fatal in asthmatics) CNS seadtion Hypoglycemia Hyperlipidemia
Highest lipid solubility B blockers
Propranolol
Nebivolol
Bisoprolol
Peanut butter N jelly it has a lot of fat
BPN
lowest lipid solubility B blockers
Atenolol
Sotalol
If you want nice ass you need to eat less fat
B blockers contraindications
Acute heart failure
Cardiogenic shcok
Careful in case of Asthma/COPD
Careful in DM
B blockers with local anesthetic effect
Acebutol
Labetalol
Metoprolol
Pindolol
Propranolol
Spasmolytic agents
Diazepam: GABA-A agonist
Baclofen: GABA-B agonist
Tizanidine: a2 agonist
Tolperisone: Inhibition of Ca2+ and Na+ ch.
Diazepam receptror preferance
GABA-A
DiAAAAAzepam
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
Diazepam metabolism and duration of action
Hepatic
12-24 h
Diazepam indications
Centrally-acting spasmolytlcs
- Chronic spasm (Cerebral palsy, stroke, spinal injury)
- Acute spasm due to muscle injury
Diazepam side effects
CNS depressant
Tolerance
Dependent liability
What is an GABA-B agonist?
Baclofen
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
Baclofen
How to give?
Oral
Intrathecal for severe spasticity
Baclofen indications
Spasm (Cerebral palsy, stroke, multiple sclerosis)
Baclofen side effects
Sedation
Weakness
Rebound spasticity when abrupt withdrawal
Spasmolytic a2 agonist
Tizanidine
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
Tizanidine indications
Spasm (stroke, multiple sclerosis)
-Oral for acute and
chronic spasms
Tizanidine side effects
Wekness Sedation Hypotension Hepatotoxiciy Rebound HTN when abrupt withdrawal
Tolperisone MOA
Inhibition of muscle stretch reflex
Reduction of muscle reflex
Oral
Hungarian
-inhibition of Na & Ca channels
Tolperisone indication
Acute spasm due to muscle injury
No used in chronic spasm
Tolperisone side effects
Sedation
Confusion
Ocular effects
Strong anti muscarinic effects
SOS-C
Direct acting muscle relaxants
Dantrolene
Botulinium toxin
Dentrolene MOA
RyR1 antagonist → Blocks Ca2+ release ch. in the Sarcoplamis reticulum of skeletal muscle → reduces actin-myosin interaction
Dentrolene
How to give? Duration?
Oral, IV
4-6 h
Dentrolene indications
- Malignant hyperthermia (IV)
- Neuroleptic malignant syndrome (NMS)
Spasm (Crebral palsy, multiple sclerosis)
-Oral for acute and chronic
spasms
Dentrolene side effects
Muscle weakness
Hepatotoxicity
Botulinium toxin MOA
Prevent synaptic exocytosis through inhibition of SNARE fusion proteins in presynaptic nerve terminals → Flaccid paralysis
Botulinium toxin
How to give? Duration?
Direct IM
2-3 months
Botulinium toxin indications
-Upper and lower limb spasm (Crebral palsy, multiple sclerosis)
- Cervical dystonia
- Migrane
- Overactive bladder
- Hyperhidrosis
Cosmetics
Non depolarizing neuromascular blocking agents
Cisatra-curium
Miva-curium
Ro-curonium
Pan-curonium
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
Atracuriun Cisatracurium Mivacurium Rocuronium Pancuronium
Which is a steroid?
Rocuronium ( Hepatic)
Pancuronium (Renal, unchanged in urine)
Atracuriun Cisatracurium Mivacurium Rocuronium Pancoronium
Metabolism
- Cisatracurium: Spontaneous breakdown (Hofmann elimination) less laudonosine
- atracurium: Spontaneous breakdown (Hofmann elimination)
- Mivacurium: Pseudocholinesterase
- Rocuronium: Hepatic
- Pipecoronium: Renal
Atracurium
cisatracurium
Mivacurium
side effects
- Histamine release (Hyotension)
- Prolonged apnea (Muscle weakness)
Laudanosine formation
(atracurium) –> provoke seizure in renal impairement
Cisatracurium side effects
Histamine release (Hyotension) Prolonged apnea (Muscle weakness)
Mivacurium SE
Histamine release (Hyotension) Prolonged apnea (Muscle weakness)
-withdrawn from market in USA
Rocuronium SE
Prolonged apnea (Muscle weakness)
Most potent neuromascular blocking agent
Pipecuronium
Depolarizing neuromascular blocking agents
Succinylcholine (Suxamethonium)
Succinylcholine
How to give? Duration of action? metabolism?
Parenteral
5 min
Rapid metabolism by plasma cholinesterase
Succinylcholine indications
Intubation
Endoscopy
ECT “electro-convulsive therapy)
Succinylcholine side effects
Arrhthmias
Hyperkalemia
Postoperative muscle pain
Malignant hyperthermia
B agonists
Sabutamol (Albuterol)
Terbutaline
Feno.terol
Salme.terol
Formo.terol
Long acting B2 agonists
Salmeterol
Formoterol
they Flow Slow
More Formal
We are Salmates
Short acting B2 agonists
Salbutamol
Terbutaline
Fenoterol
Fest, Salbation, Terter
SABA
Duration of action
Onset of action
How to give?
< 4 h
5 min
Aerosol, nebulizer, parenteral
LABA
Duration of action
How to give?
12-14 h
Aerosol, nebulizer, parenteral
Short acting B2 agonists indications
Asthma
COPD
Acute asthmatic bronchospasm
Not effective in asthma prophylaxis
B2 agonists side effects
Tachycardia
Tremor
Arrhythmia
Which B2 agonist is used to suppress premature labor
Terbutaline
LABA indications
Bronchodilation in asthma and COPD
Prophylaxis
Not effective for acute episodes
Combination with corticosteroides is good
Muscarinic antagonist used in asthma
Which is longer acting?
Tiotropium is longer acting than Ipratropium
Methylxantine used in asthma?
Theophylline (tea)
Theophylline
How to give
Duration of action
Oral
Slow onset, 12 h diration of action
Theophylline metabolism
CYP450
Theophylline MOA
PDE inhibition → cAMP↑ → Bronchodilation and reduced inflammation
Also Adenosine antagonist → CNS effects
methylxanthine used in asthma
Corticosteroides for the treatment of asthma?
Budesonide
beclomethasone
Dexamethasone
fluticasone
Prednisone (oral)
Prednisolone (I.V GC)
methylprednisolone ( oral, parenteral)
Budesonide
Dexamethasone
Duration of action
10-12 h
Prednisone
Duration of action
12-24 h
Budesonide
Dexamethasone
Prednisone
Which is oral and which is inhaled?
Budesonide: inhaled
Dexamethasone: inhaled
Prednisone: oral
Methylprednisolone is given how?
Oral
IM, SC
Methylprednisolone duration of action
12-36 h
Prednisone side effects
Systemic toxicity appear when systemic treatment > 2 weeks
Adrenal suppression, growth inhibition, muscle wasting, osteoporosis, salt retention, glucose intolerance, behavioral changes
Budesonide side effects
Oropharyngeal candidiasis
Leukotriens antagonist
Monteleukast
Monteleukast MOA
LTD4-R antagonist
- reduce inflammation
- decrease bronchoconstriction
Monteleukast
How to give? Duration of action?
Oral
12-24 h
Monteleukast indications
Asthma prophylaxis
Oral treatment in children
Minimal side effects!
Selective inhibitor of LOX enzyme
Zileuton
Anti IgE Ab
Omalizumab
Omalizumab molecule properties
human monoclonal IgG Ab against Fc region of IgE
Omalizumab
How to give?
Indications?
Parenteral
Prophylaxis for severe asthma that is not responsive for other drugs
What can we give topically for rhinitis?
Fluticasone
Which drug desensitize the stretch receptors in the lungs?
Prenoxdiazine
Prenoxdiazine
Whaat is special about it?
peripherally acting anti-tussive ( like lidocaine)
Does not cause addiction
Prenoxdiazine indications
Cough from bronchial origin
Codeine
What is it?
Duration?
Indications?
Opioid derivative
Short duration
Acute and chronic dry cough
Codeine MOA
Mue receptor agonist- Suppress cough reflex
Non opioid centrally acting antitussives
Butamirate
pentoxyverine
Butamirate indications
Cough
COPD (maybe)
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
Acetylcysteine MOA
How to give?
Reduces disulfide bonds in mucus matrix → Mucus viscosity ↓
Oral
mucolytic
Bromhexine MOA
Increase the production of serous fluid in the respiratory tract whcih maces mucus thinner and less viscous
Mucoactive agents:
Acetylcysteine
Bromhexine
Indications
CF
Chronic bronchitis
Bronchiectasis
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
Specific treatment- Peripheral Vascular Disease
5 drugs
Cilostazol Pentoxifylline Vinpocetine Nicergoline Calcium dobesilate
Cilostazol MOA
How to give
PDE-3 inhibitor → PLT aggregation ↓, Vasodilation, LPL activity ↑
Oral
Cilostazol indications and side effects
Intermittent caludication
Headache, palpitations, vertigo, coronary steal synd.
Cilostazol contraindication
CHF
congestive
heart failure because of evidence of reduced survival.
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
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
Pentoxifylline indications
Atherosclerosis circulatory disease
Diabetic circulatory disease
Intermittent caludication
Pentoxifylline side effects
GI Tachycardia Angina Cutaneous flushing Allergy
Migrane specific treatment
Sumatriptan
Sumatriptan MOA
Selective 5-HT1D/1B agonist
Sumatriptan indications
Acute migrane attack
Sumatriptan side effects
Abnormal sensation
Dizziness
Chest pain
Coronary vasospasm
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
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