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Pharmacology > Week 12: Respiratory, Eyes, Ears, and Skin Drugs > Flashcards

Week 12: Respiratory, Eyes, Ears, and Skin Drugs Flashcards

1
Q

Characteristics of inflammation (3)

A
  1. Increased vascular permeability
  2. Extravasation of WBC
  3. Swelling, warmth, redness, pain
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2
Q

Glucocorticoid MoA and effects (3)

A

MoA:
1. Enter cell via phospholipid bilayer
2. Bind to receptor-steroid complex in cytoplasm
3. Complex moves to the nucleus and binds to chromatin in DNA, altering mRNA transcription
4. Inc. or dec. in protein synthesis
Effects:
- Dec. warmth, redness, pain, and swelling at site of irritation
- Dec. bacterial killing (infection risk)
- Dec. antibody production (dec. humoral immunity)

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3
Q

Cortisone // Hydrocortisone: Class, MoA, AE (9)

A

Class: Glucocorticoid
MoA: Binds to receptor-steroid complex -> alters mRNA transcription
AE:
- Risk for infection, caution with vaccine administration
- Adrenal insufficiency
- Osteoporosis
- Hyperglycemia
- Growth delay in children
- Fluid/electrolyte disturbances
- Peptic ulcer disease
- Psychological disturbances
- Cataracts and glaucoma

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4
Q

Prednisone: Class, MoA, AE (9)

A

Class: Glucocorticoid
MoA: Binds to receptor-steroid complex -> alters mRNA transcription
AE:
- Risk for infection, caution with vaccine administration
- Adrenal insufficiency
- Osteoporosis
- Hyperglycemia
- Growth delay in children
- Fluid/electrolyte disturbances
- Peptic ulcer disease
- Psychological disturbances
- Cataracts and glaucoma

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5
Q

Dexamethasone: Class, MoA, AE (9)

A

Class: Glucocorticoid
MoA: Binds to receptor-steroid complex -> alters mRNA transcription
AE:
- Risk for infection, caution with vaccine administration
- Adrenal insufficiency
- Osteoporosis
- Hyperglycemia
- Growth delay in children
- Fluid/electrolyte disturbances
- Peptic ulcer disease
- Psychological disturbances
- Cataracts and glaucoma

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6
Q

How do exogenous glucocorticoids pose a risk for adrenal suppression?

A

Long-term therapy suppresses CRH/ACTH due to high glucocorticoid levels =
decreased adrenal synthesis/release of glucocorticoid, resulting in adrenal atrophy

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7
Q

Cyclosporine // Tacrolimus: Class, indications, MoA, AE (10), drug interactions (2)

A

Class: Calcineurin inhibitors
Indications: Transplant rejection
MoA: Inhibit calcineurin -> suppress IL-2 production = dec. T and B cell proliferation
AE:
- Nephrotoxicity (common)
- Infection (common)
- Hepatotoxicity
- Lymphoma
- Anaphylaxis
- HTN
- Tremor
- Gynecomastia
- HyperK+
- Hyperglycemia
Drug interactions:
- Avoid other nephrotoxic drugs
- CYP450 inducers/inhibitors = organ rejection or drug toxicity

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8
Q

Tacrolimus: What’s unique?

A

Somewhat more effective than Cyclosporine, but smaller therapeutic index

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9
Q

mTOR inhibitors: Indications, MoA, AE (6)

A

Indications: Kidney/renal transplant rejection
MoA: Inhibit mTOR = IL-2 inhibition = dec. T and B cell proliferation
AE:
- Infection risk
- HLD
- Myelosuppression -> Anemia, thrombocytopenia, leukopenia
- Nephrotoxicity

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10
Q

Azathioprine // Cyclophosphamide // Methotrexate // Mycophenolate mofetil: Class, MoA, AE (4)

A

Class: Cytotoxic drugs
MoA: Kills B and T cells that are undergoing proliferation
AE:
- Bone marrow suppression
- GI disturbances
- Reduced fertility
- Alopecia

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11
Q

Azathioprine: What’s unique?

A

Interferes with folate metabolism

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12
Q

Methotrexate: What’s unique?

A

Interferes with folate metabolism

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13
Q

Mycophenolate mofetil: What’s unique?

A

Selective B and T cell inhibition due to suppression of inosine monophosphate dehydrogenase

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14
Q

Antibodies: General MoA and AE (2)

A

MoA: Directed at components of the immune system = suppressed immune responses
AE:
- High risk for infection
- Hypersensitivities

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15
Q

Actions of H1 receptor agonism (7)

A
  1. Vasodilation and inc. capillary permeability (swelling, redness, warmth)
  2. HypoTN and reflex tachycardia
  3. Itching and pain (Stimulation of sensory nerves)
  4. CNS: Cognition, memory, sleep/wake
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16
Q

Diphenhydramine // Promethazine: Class, indications (3), MoA, AE (11), PK

A

Class: 1st gen H1 receptor antagonists
Indications: Mild allergy or in adjunct in severe allergy
- Motion sickness
- Insomnia
MoA: Selectively blocks H1 receptors
- Some agents can block M receptors (anticholinergic side effects)
AE:
- Sedation
- Dizziness and coordination problems
- Confusion
- Acute toxicity: Hallucination, excitation, seizures (children)
- N/V, loss of appetite
- Constipation
- Dry mouth/eyes
- Dec. DI/GU motility
- Tachycardia
- Respiratory depression at extremes of age
- Avoid use with other CNS depressants
PK: Small, highly lipid-soluble = CNS effects

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17
Q

Fexofenadine: Class, indications (2), MoA, AE (6), PK

A

Class: 2nd generation H1 receptor antagonists
Indications: Mild allergy or in adjunct in severe allergy
- Motion sickness
MoA: Selectively blocks H1 receptors
- Some agents can block M receptors (anticholinergic side effects)
AE:
- N/V, loss of appetite
- Constipation
- Dry mouth/eyes
- Dec. DI/GU motility
- Tachycardia
- Respiratory depression at extremes of age
PK: Large, polar = no BBB crossing

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18
Q

Asthma: General pathophysiology

A

Allergen binds IgE antibodies on mast cells
- Release of mediators (histamines)
- Bronchoconstriction + infiltration of inflammatory cells

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19
Q

Chronic bronchitis: Definition and general pathophysiology

A

33

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20
Q

Emphysema: Definition and general pathophysiology

A

33

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21
Q

MDI (metered dose inhaler)

A

36

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22
Q

Respimat

A

36

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23
Q

DPI (dry powder inhaler)

A

36

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24
Q

Nebulizers

A

36

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25
Considerations for bronchodilators (3)
- Bronchodilators don't alter underlying pathophysiology - Bronchodilators don't dec. inflammation - Most that use bronchodilators must use an anti-inflammatory for long-term management
26
Albuterol // Terbutaline: Class, indications, MoA, AE (5), administration guidelines (2)
Class: Short-acting B2 agonist (SABA) Indications: PRN to abort acute attack (acute bronchospasm) MoA: B2 agonism AE: - Tremors - Tachycardia/dysrhythmia → angina - Hyperglycemia - Hypokalemia - Nervousness Administration guidelines: - PO or inhaled - Also combined with cromolyn to prevent exercise-induced bronchospasm
27
Salmeterol // Formoterol: Class, indications, MoA, AE (5), administration guidelines (3)
Class: Long-acting B2 agonist (LABA) Indications: COPD MoA: B2 agonism AE: - Tremors - Tachycardia/dysrhythmia → angina - Hyperglycemia - Hypokalemia - Nervousness Administration guidelines: - PO or inhaled - Fixed dosing schedule - Should never be given alone, usually given with glucocorticoid
28
Theophylline: Class, indications, MoA, AE (5), administration guidelines (2), interactions (4)
Class: Methylxanthine Indications: COPD MoA: Block adenosine receptors AE: - CNS excitation → seizures - Cardiac stim → dysrhythmias → cardiac arrest - Vasodilation → hypotension - Diuresis - Nausea/vomiting/diarrhea Admin guidelines: - Slow IV admin to avoid fatal CV events - Monitor plasma levels Interactions: - Caffeine → increases AE - Tobacco/marijuana → induces CYP450 - CYP450 inducers → subtherapeutic theophyline levels - CYP450 inhibitors → subtherapeutic (toxic) theophyline levels
29
Ipratropium: Class, indication (1), MoA, AE
Class: Short-acting anticholinergic (SAMA) Indication: Bronchospasm MoA: Block M receptors in the bronchi AE: Quaternary ammonium → minimal AE
30
Tiotropium: Class, indication (1), MoA, AE
Class: Long-acting anticholinergic (LAMA) Indication: Long-term bronchospasm prevention MoA: Block M receptors on bronchi AE: Quaternary ammonium → minimal AEs
31
Beclomethasone // Budesonide // Fluticasone: Class, Indication, MoA (3), AE (3)
Class: Inhaled glucocorticoid Indication: Long-term control of airway inflammation MoA: - Decreased synthesis and release of inflammatory factors - Decreased infiltration of inflammatory cells - Decreased edema of the airway mucosa AEs: - Oropharyngeal candida (thrush) - Dysphonia (hoarseness) - Long term high dose therapy can have systemic AE
32
Zileuton: Class, Administration, Indication, MoA (4), AE (3)
Class: Leukotriene receptor antagonist Administration: PO Indication: 2nd line for asthma if pt can't tolerate glucocorticoids* NOT for acute attack relief MoA: - Smooth muscle constriction - Increased blood vessel permeability - Increased inflammatory response (directly + through eosinophil recruitment) - block leukotriene synthesis AEs: - Neuropsych effects (depression, SI) - Liver injury - CYP450 inhibition
33
Montelukast: Class (2), Administration, Indication, MoA (4), AE (2)
Class: - Leukotriene receptor antagonist - Highly protein bound Administration: PO Indication: 2nd line for asthma if patient can't tolerate glucocorticoids* NOT for acute attack relief MoA: - Smooth muscle constriction - Increased blood vessel permeability - Increased inflammatory response (directly and through eosinophil recruitment) - Blocks leukotriene RECEPTORS AEs: - Minimal AE - Rare neuropsych effects
34
Cromolyn: Class, Indications (3), MoA (3), AE
Class: Mast cell stabilizer Indications: - Safest of all anti-asthma drugs - Exercise induced asthma - Allergic rhinitis MoA: - Decreased histamine and mediator release - Decreased inflammation - Does NOT cause bronchodilation AE: very rare AE
35
Omalizumab: Class, Indications (2), MoA (2), AEs (4)
Class: Monoclonal antibody IgE antibody antagonist Indications: - Not first line drugs; none for acute management - For serious uncontrolled asthma MoA: - Forms complex with IgE that prevents binding - Decreased inflammatory mediator release AEs: - Vital infections - Injection site reactions → hypersensitivity reactions - 1/2 life = 26 days, takes 1yr to return to pre-drug levels - Increased risk of infection for ~1 yr after admin
36
Monoclonal antibody: Interleukin-5 receptor antagonist: Class, Indications (2), MoA (2), AE (5)
Class: IL-5 receptor antagonist Indications: - Not first line drugs; none for acute management - For serious uncontrolled asthma MoA: - Inhibit IL-5 - Decreased eosinophils AE: - Headache - Pharyngitis - Fatigue - Hypersensitivity reactions - Anaphylaxis (RESLIZUMAB)
37
Monoclonal antibody: Interleukin-4 receptor antagonist: Class, Indications (2), MoA (2), AE (4)
Class: IL-4 receptor alpha antagonist Indications: - Not first line drugs; none for acute management - For serious uncontrolled asthma MoA: - Inhibit IL-4 - Decreased cytokine-induced inflammation AE: - Injection site reaction - Oral herpes - Conjunctivitis - Antibody development against the drug
38
Roflumilast: Class, Distinguishing features (2), Indications, MoA (4), AE (6), Contraindication (1)
Class: PDE4 inhibitor Distinguishing features: - PO - 1/2 life 17 hours due to high protein binding Indication: Severe bronchitis primary COPD (not first line) MoA: - Inhibits PDE4 - Increased cAMP - Suppression of cytokines - Decrease WBC infiltration AE: - Diarrhea - Anorexia - Headache - Back pain - Insomnia - Severe psych reactions Contraindication: avoid in pregnancy
39
SYMBICORT
Budesonide / Formoterol
40
ADVAIR
Fluticasone propionate / Salmeterol
41
COMBIVENT
Albuterol / Ipratropium
42
Phenylephrine // Pseudoephedrine: Class, Administration, Indication (2), MoA (4), AE (2), Contraindications (1)
Class: Sympathomimetic A1 agonist Administration: Intranasal Indication: - Allergic rhinitis - Allergic conjunctivitis MoA: - A1 agonism in nasal vessels - Vasoconstriction - Decreased vascular swelling and permeability - Effects are rapid and intense AE: - CNS stimulation + CV effects at high doses - Rebound congestion Contraindications: Can be readily converted into meth
43
Guiafenesin: Class, MoA
Class: Expectorant MoA: Promote sputum to expel stuff from lungs
44
Hypertonic saline // Acetylcysteine (inhaled): Class, MoA
Class: Mucolytics MoA: Break down thick mucus
45
Codeine // Hydrocodone: Class, MoA, Distinguishing factors (3)
Class: Opioid antitussive MoA: Act in CNS to elevate cough threshold Distinguishing factors: - Risk for physical dependence is small - Can still cause respiratory depression - Formulated with other meds to decrease abuse potential
46
Dextromethorphan: Class, MoA, Distinguishing factors (2)
Class: Non-opioid antitussive MoA: CNS actions Distinguishing factors - At high doses → euphoria (can be abused) - NO respiratory depression
47
Timolol: Class, Administration, Indication, MoA, AE (1)
Class: Beta blocker Administration: locally (eyedrops) Indication: Glaucoma MoA: Decrease aqueous humor production AE: Systemic beta blockade
48
Latanoprost: Class, Administration, Indication, MoA (2), AE (1)
Class: Prostaglandin analogs Administration: locally (eyedrops) Indication: Glaucoma MoA: - Increases AH outflow - Relaxes ciliary muscle AE: Ocular hyperemia (enlarged vessels)
49
Brimonidine: Class, Administration, Indication, MoA, AE (2)
Class: Alpha 2 agonist Administration: locally (eyedrops) Indication: Glaucoma MoA: Decreases AH production AE: - Dry mouth - Ocular hyperemia
50
Dorzolamide: Class, Administration, Indication, MoA
Class: Carbonic anhydrase inhibitors Administration: locally (eyedrops) Indication: Glaucoma (least effective) MoA: Decreases AH production
51
Azelastine: Class, Indication, MoA
Class: H1 receptor blocker Indication: Allergic conjunctivits MoA: Prevents mast cell activation
52
Bevicizumab: Class, Administration, Indication, MoA (2)
Class: VEGF inhibitor Administration: Injected DIRECTLY into vitreous humor Indication: Age related macular degeneration (WET ONLY) MoA: - Prevents VEGF from binding to receptors - Prevents angiogenesis
53
Hydrocortisone // cortisone (SKIN): Class, Indication, AE (2)
Class: Topical glucocorticoids Indication: Rash/itching AE: - Local reactions - Thinning of skin with long-term use
54
Salicylic acid: Class, Indications (5), AE (1)
Class: Keratoytics Indications: - Overgrowth/thickening - Dandruff - Psoriasis - Warts - Corns AE: Toxicity with long-term and high-dose use (RARE)
55
Benzoyl Peroxide: Class, Indication, AE (2)
Class: Topical antibiotics Indication: Acne (first line) AE: - Peeling - Drying
56
Tretinoin: Class, Indication, MoA (2), AE (2)
Class: Retinoids Indication: Acne MoA: - Vit A derivatives - Hyper proliferation of epithelial cells AE: - Peeling - Drying
57
Methotrexate: Class, Indication, Contraindication (1)
Class: Systemic Indication: Psoriasis Contraindication: Pregnancy
58
Topical tracrolimus: Class, Indication, MoA
Class: Immunosuppressant Indication: Eczema (2nd line) MoA: No systemic absorption
59
Topical minoxidil: Class, Indication, MoA, AE (1)
Class: Direct vasodilator Indication: Hair loss MoA: Unknown (maybe increased blood flow) AE: Local allergic reactions
60
Amoxicillin: Indication (3)
Indication: Otitis media - Infants <6m - 6m-2yr with confirmed disease - >2y with diagnosis AND severe symptoms
61
Acetic Acid: Indication (1)
Otitis externa

Pharmacology (15 decks)

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