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Pulmonary Drugs
Drugs
85
Pharmacology
Graduate
10/13/2011

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Term
Effect of Angiotensin on blood vessels
Definition
Vasoconstriction by acting on AT receptors
(Angiotensin is a peptide formed with the help of ACE)
Term
Effect of Endothelin on blood vessels
Definition
Vasoconstriction by acting on ET-A receptors
(ET-B would induce vasodilation via NO)
Is a peptide fomred in the endothelium
Mediates vascular spasm
Term
Effect of Bradykinin on blood vessels
Definition
Increases vascular permeability (involved in angioedema)
A polypeptide.
Use B2 blocker 'icatibant' to treat too much Bradykinin
Term
Effect of Prostaglandin on blood vessels
Definition
Vasodilation
Is derived from lipids/fatty acids
Could also induce labor when acting on uterine tissue.
Term
Antihistamines
(Effect on receptor)
(Structural importance)
(Distribution)
(Receptors affected)
Definition
Effect: Inverse Agonist on H-1
Structural/Distribution: 1st generation will cross BBB. 2nd generation will not.
Receptors blocked: H-1, 5-HT, Muscarinic, DA, Alpha-adrenergic,
Term
Antihistamines
(Metabolism)
(Action)
(Use)
(ADRs)
Definition
Metabolism: FGAH~Microsomal ; SGAH~CYP3A4
Action: CNS~Sedation ; Lungs~Blocks hypersecretion and bronchoconstriction ; Vessels~Vasoconstriction ; Sodium channels~Inhibits ; Inflammation~Inhibits
Term
Antihistamines
(Use)
(ADRs)
(Drug Interactions)
Definition
Use: Allergy (rhinits, urticaria, dermatitis) ; Nausea/Vomiting ; Parkinson's(Benztropine); Local anesthetic(Diphenhydramine, promethazine); Dystonia
ADRs: Sedation; Dizziness; Fatigue; convulsion in children; Anti-Ach; Coma and teratogenicity
Drug Interactions: Grapefruit; Anti-ach; Alpha-block; Ketoconazole
Term
Zafirulast
Definition
Leukotriene Receptor Inhibitor(LTC4, LTD4, LTE4)
For children >5
Longer half-life than Montelukast
CYP2C9 -> Biliary excretion
Oral
Term
Montelukast
Definition
Leukotriene Receptor Inhibitor(LTC4, LTD4, LTE4)
For children >2
Shorter half-life than Zafirulast
CYP2C9 -> Biliary excretion
Oral
Term
Zileuton
Definition
Leukotriene Synthesis Inhibitor (5-lipoxygenase)
Shorter half-life than Montelukast and Zafirulast
CYP1A2,2C9,3A4 -> Urinary elimination
Oral
Term
Ranitidine
Definition
H2 Receptor Block
Used for mild GERD to decrease acid secretion
Term
Cimetidine
Definition
H2 Receptor Block
Used for mild GERD to decrease acid secretion
Term
Nizatidine
Definition
H2 Receptor Block
Used for mild GERD to decrease acid secretion
Term
Famotidine
Definition
H2 Receptor Block
Used for mild GERD to decrease acid secretion
Term
Thioperamide
Definition
H3 Receptor Antagonist
For: Sleep Disorder(Narcolepsy); Obesity; Cognitive disorder; ADHD
Other uses: As an antipsychotic for schizophrenia; ADHD
Term
Effect of Adenosine on the respiratory system
Definition
Inflammation, bronchoconstriction
Term
Effect of Adrenergic on the respiratory system
Definition
Bronchodilation (Beta 2)
Term
Effect of Cholinergic on the respiratory system
Definition
Bronchoconstriction, Increased Secretions (M-3)
Term
Effect of Leukotriene on the respiratory system
Definition
Bronchoconstriction, Inflammation (LT)
Term
Effect of Dopaminergic on the respiratory system
Definition
Decreased pulmonary vascular resistance and pulmonary HTN
Term
Effect of Histaminergic on the respiratory system
Definition
Bronchoconstriction, Increased secretion (H1)
Is NOT a mediator of asthma however.
Term
Effect of Endothelin on the respiratory system
Definition
Vasoconstriction, Pulmonary HTN
Term
Effect of Thromboxane on the blood vessels
Definition
Mediates vascular spasm
Term
What is the major ADR of Fenfluramine (Fen-Phen)
Definition
Pulmonary HTN
Is an appetite suppressant
However, its metabolite, norfenfluramine is a 5HT-2B agonist that affects the heart.
Term
Epoprostenol
Definition
Vasodilation (Prostacyclin-Naturally occuring PG)
Parenteral (IV) ; Expensive
Infection risk
For Pulmonary HTN
Term
Treprostinil
Definition
Vasodilation (Prostacyclin-synthetic)
Parenteral (SC)
Less infection risk than Epoprostenol.
For Pulmonary HTN
Term
Beraprost
Definition
Vasodilation (Prostacyclin-synthetic)
Oral
Less infection risk than Epoprostenol.
More safety and compliance
For Pulmonary HTN
Term
Bosentan
Definition
Endothelin-A Receptor antagonist (Synthetic) -> Vasodilation
Oral
For Pulmonary HTN
Term
Sildenafil (20mg) "Revatio"
Definition
Phosphodiesterase-5 inhibitor -> Vasodilation
Oral
ADRs: CNS~Amnesia, seizure; Eye~Blue vision, optic neuropathy; CVS~Ischemia
For Pulmonary HTN (As opposed to Viagra 50 mg which is for Erectile Dysfunction)
Term
Dipyridamole
Definition
Binds prostacyclines to increase their effect and will inhibit phosphodiesterase. This leads to vasodilation that can alleviate Pulmonary HTN. (Also is used as inhibitor of platelet aggregation)
Term
Apomorphine
Definition
A Dopamine Agonist
Can be used to treat Erectile Dysfunction
Term
Alprostadil
Definition
A prostaglandin.
Can be used to treat Erectile Dysfunction
Term
Phentolamine
Definition
Alpha 2 agonist
Can be used to treat Erectile Dysfunction
Term
Effect of alcohol/cocaine on Erectile Dysfunction
Definition
They can lead to decreased testosterone and thus to impotence.
Term
Methacholine
Definition
A muscarinic agonist.
Can test for Cystic Fibrosis by testing for hyper-responsiveness.
Term
Dornase
Definition
Recombinant Human deoxyribonuclease
Breaks down DNA in the sputum, decreasing its viscosity.
Used to loosen mucus in Cystic Fibrosis
Term
Hypertonic Saline
Definition
Used to loosen mucus in Cystic Fibrosis
Term
N-Acetylcysteine
Definition
Used to loosen mucus in Custic Fibrosis
Term
Alternate Treatments for Cystic Fibrosis
Definition
CFTR Gene therapy: In vivo(gene direct to organ); Ex vivo (Removal of marrow, treat with vector, replace marrow)
Transplantation: Both lungs; liver; pancrease.
Antibiotics, NSAIDS, Steroids
Vitamins A,D,E,K
High calorie diet
Calcium, electrolytes
Embryo transfer, or intracytoplasmic sperm injection for pregnancy
Term
How do you treat Nocturnal Asthma?
Definition
With Beta Adrenergic Agonists to fix the offset of catecholamines that occurs at night.
Term
Effect of cAMP on Bronchus
Definition
Bronchodilation, Hypersecretion,
(Beta-2 is Gs that increases cAMP but results in inhibition rather than stimulation when on smooth muscle)
One could also use PDE Inhibitors/Xanthine derivatives to increase cAMP.
Term
Cromolyn
Definition
Membrane stabililzer of mast cells, basophils, and inhibits release of LT/SRSA.
(Nasal, oral) For Asthma and Congestion.
Derived from Amni Visnaga(plant)
ADRs: Dermatitis, Gastroenteritis, Myositis
Term
Glucocorticoids
Definition
Inhibits PLA2, blocking PG and LT synthesis
Decreases inflammation and suppresses eosiniphil production in bone marrow.
ADRs: HTN, DM, GI bleed, Thinning of skin, Osteoporosis,
Term
Beta-Agonists
Definition
Bronchodilator via Beta-2 -> Increased cAMP
(Oral, Inhaled)
cAMP will bronchodilate, decrease vascular permeability, and suppress the parasympathetic effect
ADRs: Increased Cardiac effect, HTN, tremor, restlessnes, tachycardia, Beta receptor desensitization over chronic use.
Term
Methylxanthine
Definition
Bronchodilation via PDE inhibition, which increases cAMP, and the adenosine receptor is also blocked.
Lethal if overdosed.
ADRs: GI heartburn, Nausea, vomiting, CNS~Headache, anxiety, tremor, insomnia
e.g. Thephylline/Aminophylline
Used in COPD/Asthma
Term
Theophylline/Aminophylline
Definition
Bronchodilation via PDE inhibition, which increases cAMP, and the adenosine receptor is also blocked.
Lethal if overdosed.
ADRs: GI heartburn, Nausea, vomiting, CNS~Headache, anxiety, tremor, insomnia
Used in COPD/Asthma
Term
Ipratropium
Definition
Muscarinic Blocker.
Not as effective as Beta-agonist for controlling asthma.
ADRs: Same as all muscarinic blockers
Term
Tiotropium
Definition
Muscarinic Blocker.
Not as effective as Beta-agonist for controlling asthma.
Longer duration of action as compared to Ipratropium.
ADRs: Same as all muscarinic blockers
Term
Omalizumab
Definition
Monoclonal Antibody, Will decrease the Mast cell release of Leukotrienes.
Term
Nifedipine
Definition
Calcium channel blocker
Will act as as smooth muscle relaxant, and decrease bronchoconstriction by blocking Ca++ influx.
Term
Potassium Channel Openers
Definition
Suppress bronchoconstriction, hypersecretion, cough, airway hyperactivity,
Term
Gold
Definition
Anti-inflammatory
Term
To be avoided in Asthma
Definition
Beta Blockers, Blood Pressure Medications, Sleeping pills, tranquilizers, heart drugs, Cholinomimetics, ACE inhibitors, Analgesics, Sedatives, Anesthetics, Alcohol, Levodopa
Term
COPD Therapy
Definition
Beta Adrenergic Agonists, Anti-Cholinergics, Glucocorticoids, Methylxanthines, Long-term oxygen, Antibiotics, Alpha-Antitrypsin deficiency, Mucolytics, Narcotics, Respiratory Stimulants, Dietary Supplements, PDE Inhibitors,
Term
Almitran
Definition
Respiratory Stimulant used in COPD
Term
Doxapam
Definition
Respiratory Stimulant used in COPD
Term
Cilomilast
Definition
Respiratory Stimulant used in COPD
Term
Saline
Definition
To irrigate and smoothe irritated tissue in Congestion
Term
Oxymetazoline
Definition
Nasal Alpha-1 Adrenergic Agonist used as a decongestant
Longest Duration
Term
Naphazoline
Definition
Nasal Adrenergic Agonist used as a decongestant
Not for pediatric use
Term
Phenylephrine
Definition
Nasal Alpha-1 Adrenergic Agonist used as a decongestant
Shortest duration
Term
Nasal Corticosteroids
Definition
2-3 days to exert its effect. Must not sneeze for 10 minutes after applying.
Mechanism: Inhibits lipocortin synth. which inhibits prostaglandin production.
ADRs: Nose~Sneezing, Bleeding, Irritation/ulceration, crusting ; Head~Headache
Term
Nasal Dexamethasone
Definition
Corticosteroid Decongestant
Low potency, high systemic absorption
Term
Nasal Beclomethasone
Definition
Corticosteroid Decongestant
Good potency, low systemic absorption
Term
Nasal Budesonide
Definition
Corticosteroid Decongestant
High potency, low systemic absorption
Term
Nasal Flunisolide
Definition
Corticosteroid Decongestant
Low potency, high systemic absorption
Term
Nasal Cromolyn
Definition
Decongestant. Cell membrane stabilizer of mast cells to inhibit degranulation.
ADRs: Local irritation, itching, burning, tingling, stinging, sneezing
Compliance: 3-4 times/day. Deep breath to inhale during congestion. Must not sneeze for 10 mintues. takes 2-4 weeks for effect.
Term
Nasal Ipratropium
Definition
Decongestant. Anticholinergic, reduced secretions.
ADRs: Nasal dryness, bleeding, headache. Low systemic ADRs.
Term
Systemic Decongestants
Definition
Delayed onset, Longer duration, no nasal irritation or rebound vasodilation.
Adrenergic ADRs: Tachycardia, Nervousness, Insomnia, Excitability, Dizziness, Tremor, Drowsiness, Nausea,
Corticosteroid ADRs: Weight gain, Diabetes Mellitus, Osteoporosis, Cataracts, Glaucoma
Term
Pseudoephedrine
Definition
Adrenergic Systemic Decongestant
Promotes Nasal/sinus drainage,
Formulations: Cap, Tab, Liquid, Syrup
DIs: MAOI,
Counseling: Do not crush ER tab, and do not exceed recommended dose.
Term
Ephedrine
Definition
Adrenergic Systemic Decongestant/bronchodilator
Formulation: Cap, Injection, Jelly, Spray,
Caution in cardiovascular patient
DIs: MAOI, Theophylline
Term
Phenylpropanolamine
Definition
Adrenergic Systemic Decongestant
For Temp. relief, weight loss
Low Therapeutic Index********
Term
Explain Immunotherapy
Definition
Administration of gradually increasing concentration of an aggravating allergen to increase tolerance to the allergen.
Very expensive and patient must be compliant(patience and regular hospital visits)
Contra: HIV, AIDS, Auto-immunity, Pregnancy, Beta-blockers
Term
Disadvantages of morphine for cough
Definition
Even though it has anti-tussive properties by acting on a non-opiod receptor, there is still liability, euphoria, respiratory depression, and analgesia from the opiod receptor.
Term
Codeine/hydrocodeine
Definition
Morphine derivatives. Methylation of phenolic group and alteration of the C-ring. Codeine has anti-tussive effect without the analgesic property (some remains with hydrocodone. Sedative effects are also present (more so with hydrocodone)
Term
Benzonatate
Definition
Non-opiod Peripheral Cough suppressant
Local anasthetic that acts on stretch receptors(on alveoli/bronchi).
More effective than codeine
ADRs: Headache, mental confusion, sedation
Term
Tetracaine
Definition
Non-opiod Peripheral Cough suppressant
Local anasthetic that acts on stretch receptors(on alveoli/bronchi).
More effective than codeine
ADRs: Headache, mental confusion, sedation
Term
Dextromethorphan
Definition
Anti-tussive. Morphine derivative.
Preferred over codeine for cough suppression.
Term
Furosemide
Definition
Therapy of pulmonary edema
Term
Nitroprusside
Definition
Therapy of pulmonary edema
Term
Symptoms and Therapy of Pharyngitis
Definition
Sore throat, Fever, Dysphagia
No Cough
Therapy: Antibiotics
Term
Symptoms and Therapy of Sinusitis
Definition
Muco-ciliary epithelium affected, nasal discharge, facial pain, fever
Therapy: Antibiotics, No decongestants
Term
Symptoms and Therapy of Epiglottis
Definition
(The 4D's)Dysphagia, Drooling, distress, dysphonia, fever
Therapy: Antibiotics, Moist Oxygen
Term
Symptoms and Therapy of Laryngitis
Definition
Barking Cough
No Drooling
Therapy: Antibiotics, Dehumidified air, Epinephrine, Glucocorticoids.
Term
Therapy for Cardiopulmonary arrest
Definition
Non-Pharmacological: CPR, electrical defibrillation
Pharmacological:
Epinephrine,
Vasopressin(ADH) to vasoconstrict and increase BP,
Antiarrhymics like lidocaine, and amiodarone
Thrombolytics
Atropine
Magnesium
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