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Pharmacology - Block 2 - Part 4

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davidwurbel7's version from 2016-07-03 07:08

Bronchial Asthma

Question Answer
The main chemical mediator for the symptoms of Asthma is thisLeuktrienes
Adrenergic agonists - Albuterol, Terbutaline, Salmeterol, Formeterol; Methylxanthines - Theophylline; Muscarinic antagonists - Ipratropium bromideBronchodilators
Inhaled Cortico Steroids (ICS); Systemic Cortico Steroids; Leukotriene antagonists - Zafirlukast, Montelukast, Zileuton; Mast cell stabilizers - Cromolyn & Nedocromil; Anti-Ig E monoclonal antibody - OmalizumabControllers
β2 Agonists have minimal or no adverse drug reactions when delivered by this routeInhaled
The mechanism of action of β2 agonists to increase thisCyclic AMP
Adverse drug reactions include tolerance, fine tremors, palpitation, dizziness, restlessness, agitation and hypokalemiaβ2 Agonists
Short acting (SABA) used only for symptomatic relief in acute managementAlbuterol (Salbutamol)
Long acting (LABA) used for prophylaxisSalmeterol
Short-acting beta-2 agonist. Duration is short. Used As-needed in maintenance of chronic asthma. Used for treatment of acute asthma because of its quick onset of action. Chances of tolerance development is higherAlbuterol
Long-acting beta-2 agonist, Duration 12 hours. Used for Prophylaxis (inhalation). Not used for treatment of acute asthma due to delayed onset of action. Chances of tolerance development is lesserSalmeterol
Short acting, muscarinic antagonists, slower response. Increase the mucociliary clearance. Used as solutions in nebulisers or inhalers. DOC used in COPD. Used as an adjuvant to β2 agonists and corticosteroids in acute asthmaIpratropium Bromide
This is the drug of choice for treatment of COPDIpratropium Bromide
Long-acting, muscarinic antagonists. Increase the mucociliary clearance. Used as solutions in nebulisers or inhalers. DOC used in COPD. Used as an adjuvant to β2 agonists and corticosteroids in acute asthmaTiotropium
Methylxanthine that inhibits Phosphodiesterase (PDE) and causes bronchodilationTheophylline
Slow release useful in nocturnal asthma. Used as an add on drug, where inhaled steroid plus beta agonists are ineffectiveTheophylline
Has a narrow therapeutic margin - bronchodilator effect at 5-20mg/L - Increasing side effects > 25mg/L and therefore requires therapeutic drug monitoring (TDM)Theophylline
Used as an add on drug, where inhaled steroid plus beta agonists are ineffectiveTheophylline
Reduce Bronchial hyperactivity. Reduce the Mucosal edema. Increase the responsiveness of beta receptors on the airwayInhaled Corticosteroids (ICS)
This class of drug have only the anti-inflammatory effects. Have no direct bronchodilator effect. Have no role in the treatment of acute bronchoconstrictionInhaled Corticosteroids (ICS)
This class of drug have very few adverse effects such as dysphonia and oropharyngeal candidiasisInhaled Corticosteroids (ICS)
This can be prevented by advising the patient to gargle the mouth with saline water after use of Inhaled Corticosteroids (ICS)Oropharyngeal Candidiasis
The mechanism of action of this class of drugs include modulation of cytokine and chemokine production , inhibition of eicosanoid synthesis, inhibition of accumulation of mast cells and decrease in vascular permeability. Actions: reduce Bronchial hyperactivity, reduce the Mucosal edema and increase the responsiveness of beta receptors on the airwayInhaled Corticosteroids (ICS)
The use of this class of drugs in an asthma patient can precipitate asthma attacksNSAIDs
NSAIDs precipitate asthma attacks because they block this enzyme pushing more archodonic acid into production of leukotrienesCOX
NSAIDs precipitate asthma attacks because they block COX pushing more archodonic acid into production of thisLeukotrienes
Beclomethasone, Budesonide, Fluticasone and Triamcinolone are examples of this class of drugsInhaled Corticosteroids (ICS)
Indications for systemic steroids - Severe chronic asthma - recurrencesPrednisolone (Oral)
Indications for systemic steroids - Status asthmaticusMethylprednisolone (IV) or Hydrocortisone (IV)
A 5-lipoxygenase inhibitor. Used in Aspirin induced asthma. Toxicity - Elevation of liver enzymesZileuton
If asthma attack is induced by use of an NSAID, this class of drug should be usedLeukotriene Synthesis Inhibitor
The Leukotriene synthesis inhibitor that is most used in NSAID induced asthmaZileuton
These do not act as bronchodilators and do not cause smooth muscle relaxation. Only anti-inflammatory effects. Act by stabilizing the mast cell from degranulation and inhibiting the further release of inflammatory mediators from the mast cell. They are given orally and usually are very safe, poor bioavailabilityMast Cell Stabilizers
This class of drug can be used as prophylaxis of asthma, allergic rhinitis and conjunctivitisMast Cell Stabilizers
Humanized monoclonal antibody to human IgE. Inhibits the binding of IgE to mast cells. Prevents release of mediators. Used as a prophylaxis of asthmaOmalizumab
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Sedative-Hypnotics-Anxiolytic Drugs

Question Answer
The ability of these agents to calm or reduce anxiety, known as an anxiolytic effectSedative
The ability of these agents to induce drowsiness and encourage the onset and maintenance of a state of sleep. Hypnotic effects involve more pronounced depression of the CNS than sedationHypnotic
Alprazolam, Chlordiazepoxide, Clonazepam, Diazepam, Flurazepam, Lorazepam, Midazolam, Oxazepam, Temazepam, Triazolam are examples of this class of drugsBenzodiazepines
Amobarbital, Pentobarbital, Phenobarbital, Secobarbital, Thiopental are examples of this class of drugsBarbiturates
Buspirone, Propranolol are examples of this class of drugsNon-sedating Anxiolytic Drugs
Zolpidem, EsZopiclone, Zaleplon are examples of this class of drugsNewer Hypnotics (Z-Drugs)
Ramelteon is an example of this class of drugsMelatonin Receptor Agonists
Pentameric membrane protein containing an ion channel selective for chloride ionsGABAa Receptor
GABAa receptor is an ion channel for this ionChloride Ions
GABA binds at this place on the GABAa receptora/b Interface.
Benzodiazepines and newer drugs like zolpidem bind at this place on the GABAa receptorAlpha/Gamma Interface
This drug is used in toxicity of BenzodiazepinesFlumazenil
This drug is used in toxicity of Z-drugsFlumazenil
The mechanism of action of this class increased frequency of chloride channel openingsBenzodiazepines
The mechanism of action of this class prolong duration of chloride channel openingsBarbiturates
This barbiturate is highly lipid soluble, rapid onset of action and short durationThiopentone
This benzodiazepine is highly lipid soluble, rapid onset of action and short durationTriazolam
The duration of action of Chlordiazepoxide, Diazepam, Prazepam, and Clorazepate is thisLong Acting
The duration of action of Oxazepam, Temazepam, Lorazepam, Alprazolam and Triazolam is thisShort Acting
The duration of action of Zolpidem and Zaleplon is thisShort Acting
These drugs also exert dose-dependent anterograde amnesic effectsBenzodiazepines
Benzodiazepines and Z-drugs are use for treatment forInsomnia
Promote sleep onset and increase the duration of the sleep state. Shortens time taken for onset of sleep increase stage 2 NREM Sleep duration. Duration of REM sleep is decreasedBenzodiazepines and Z-drugs
The drug of choice for Status epilepticusDiazepam or Lorazepam
This drug is effective at sedative dose levels of skeletal muscle relaxationDiazepam
Decrease in responsiveness, commonly occurs when sedative-hypnotics are used continuously. Requires higher dosage to achieve the same responseTolerance
Frequently with most sedative-hypnotics due their anti-anxiety, euphoric, disinhibitory and sleep-inducing effectsPsychologic Dependence
An altered state that requires continuous use of the drug to prevent an abstinence or withdrawal syndromePhysical Dependence
These may include effects opposite to the action of the drug, anxiety, tremors, hyper-reflexia → to seizuresWithdrawal Symptoms
The intensity of withdrawal symptoms is dependent on this characteristic of a drugHalf-Life
This drug can be used for alcohol withdrawal symptomsDiazepam
The drug used for generalize axiety, there is an unlikely dependenceBuspirone
Buspirone acts as an agonist on this receptorSerotonin Receptor
DOC for status epilepticus, muscle spasms, tetanus, IV General Anesthesia, febrile convulsions (per rectal route ), chronic alcohol withdrawalDiazepam / Lorazepam
DOC for Panic disorders and some phobiasAlprazolam
Preanesthetic medication, IV General AnesthesiaMidazolam
For insomniaTriazolam or Zolpidem or Eszopiclone
Safer in old age patients with insomnia because they do not form active metabolitesOxazepam, Lorazepam and Temazepam
Used for DATE RAPEFlunitrazepam
Acute Anxiety DisordersPropranolol (fast acting)
Panic Disorder1) Alprazolam / Clonazepam (immediate), 2) SSRI (long term)
Phobic Disorders (most common)Benzodiazepines or SSRI
Obsessive-Compulsive Disorder (OCD)SSRI eg Sertraline or TCA, eg Clomipramine
Generalized Anxiety Disorder (GAD)Benzodiazepines for immediate relief plus Buspirone or Venlafaxine (longer term)
Toxicity symptoms include Drowsiness and lethargy— most common. Impaired psychomotor performance. Increased reaction times (slower responses). Motor incoordination. ConfusionBenzodiazapines
Withdrawal effects of rebound increase in REM sleep, Daytime sedation/depression. Tolerance. Cross tolerance with alcohol. Anterograde amnesia. Physical and psychological dependence– only on long term useBenzodiazapines
Toxicity symptoms include Withdrawl signs of anxiety, agitation. They are enzyme inducers. May precipitate acute intermittent porphyriaBarbiturates
Most are pregnancy category D, some are pregnancy category XBenzodiazepines and Barbiturates
These drugs are pregnancy category CZ-Drugs
This drugs is pregnancy category BBuspirone
Additive CNS depression when used with other CNS depressant drugs - narcotic analgesics, anticonvulsants, antihistamines, tricyclic antidepressantsBenzodiazepines
An agonist at MT1 and MT2 melatonin receptors. Used in management of insomniaRamelteon
These drugs are inducers of CYP so drug interactions can be seen with drugs that are metabolized by CYP enzymesBarbiturates
The active metabolite of Chlordiazepoxide, Diazepam, Prazepam, and Clorazepate is long acting with a half-life of 40 - 140 hoursDesmethyldiazepam
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