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Pharmacology > Antihistamines, Antifungals, Antivirals > Flashcards

Antihistamines, Antifungals, Antivirals Flashcards

1
Q

Sources of Histamine:

A
  1. Mast Cells (intestinal mucosa, skin and lungs)
  2. Basophils (in blood bound to heparin)
  3. CNS in neurons (in synaptic vesicles)
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2
Q

Mechanism of H1 antihistamines:

A

Competitive blockade of H1 receptors (H1 receptor blockers)

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3
Q

Pharmacologic effects of H1 antihistamines:

  1. Absorption
  2. Onset
  3. Duration
  4. Metabolism
A
  1. Well absorbed orally
  2. Rapid onset = 15-30 minutes
  3. Duration = 3-6 hours
  4. Metabolism primarily by over (some kidney)
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4
Q

How do H1 antihistamines affect the CNS?

A 
Produce depression (Sleepiness)
Treat motion sickness
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5
Q

What is the action of H1 antihistamines on the Autonomic nervous system and Peripheral nervous system respectively?

A

ANS: Blocks constriction of respiratory smooth muscle

PNS: Blocks flare (wheals) and itch

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6
Q

3 Adverse effects of H1 antihistamines:

A
  1. Most cause sleepiness/drowsiness
  2. Xerostomia (dry mouth)
  3. Dry mucous membranes
  • Older antihistamines caused ventricular arrhythmias
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7
Q

2 types of Antihistamines

A
  1. Ethanolamines
    - diphenhydramine (Benadryl)
  2. Alkylamines
    - chlorpheniramine (Chlor-Trimeton)
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8
Q

Name 3 non-sedating antihistamines

A

Ioratadine (Claritin) - OTC
fexofenadine (Allegra) - OTC
desloratadine (Clarinex)

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9
Q

Mechanism of action for H2 antihistamines:

A
  1. Competitive blockage of H2 receptors (GI tract)
    - Reduces intracellular concentration of cAMP
    - Protein kinase that drives the H+/K+-ATPase pump is shut down
    * *-Inhibits basal and nocturnal gastric acid secretion (evoked by histamine)
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10
Q

Pharmacologic effects of H2 Antihistamines:

  1. Absorption
  2. Metabolism
  3. If added to H1 blockers???
A
  1. Well absorbed orally
  2. Very little metabolism
  3. If aded to H1 blockers, blocks all cardiovascular effects of histamine
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11
Q

4 clinical uses of H2 Antihistamines:

A
  1. Peptic ulcer
  2. Hypersecretion of gastric acid
  3. GERD
  4. Zollinger-Ellison syndrome (gastrin producing tumor causing hypersecretion of stomach acid)
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12
Q

Name 4 H2 Antihistamines:

A
  1. cimetidine (Tagamet)
  2. famotidine (Pepcid)
  3. nizatidine (Axid)
  4. ranitidine (Zantac)
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13
Q

Adverse effects of H2 Antihistamines

A
  1. Minor
  2. Chronic use of these drugs is associated with headache, dizziness and fatigue
  3. Elderly = confusion, slurred speech, delirium and hallucinations
  4. Gynecomastia in males
  5. Impotence; 40% decrease in sperm count
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14
Q

What is the safest and most recommended drug in H2 Antihistamine class?

A

ranitidine (Zantac)

  • Fewest drug interactions
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15
Q

Which drug of the H2 Antihistamine class has the most adverse reactions

A
  1. cimetidine (Tagamet)
    - Inhibits cytochrome P450 to slow the clearance and increases the serum levels of many drugs
    - increases risk for overdose reactions
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16
Q

What is cromolyn (Gastrocrom)?

A

A mast cell stabilizer

- Inhibits degranulation, preventing histamine release from IgE sensitized mast cells

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17
Q

What is cromolyn (Gastrocrom) used for?

A

Prophylaxis of allergies, exercise-induced asthma, and asthma

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18
Q

Describe when to use topical vs systemic anti fungal treatment

A

Systemic: chronic, extensive mucocutaneous candidiasis

Topical: Local candidiasis
- **May be used in conjunction with topical corticosteroids to manage inflammation

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19
Q

Which of the anti fungal therapies is preferred?

A

Topical versus systemic is preferred

20
Q

How long to treat during anti fungal therapies

A

Treat for a minimum of 48 hours after symptoms subside
- usual treatment period is for 1-2 weeks

Re-evaluate at 14 days after therapy

21
Q

4 topical antifungal agents

A
  1. Liquids
  2. Troches
  3. Pastilles
  4. Powders
22
Q

nystatin (Mycostatin) mechanism of actions

A

Binds to sterols in fungal cell membrane, changing cell wall permeability allowing for leakage of cellular contents
-Topical

23
Q

nystatin comes in what forms?

A
  • pastilles/troches = 4-5 troches/day for 14 days
  • oral suspension = 1 tsp 4-5 times/day; rinse and hold in mouth for 2 minutes; do not eat/drink afterwards for 30 minutes; soak dentures
  • ointment/cream = 4-5 times per day; may be applied to dentures prior to insertion
  • powder = sprinkle over dentures prior to insertion 4-5 times per day
24
Q

When is clotrimazole (Mycelex) used?

A

when nystatin is not effective

- Not for systemic fungal infections. Topical use only

25
Q

Describe dosages of different forms of clotrimazole (Mycelex)

A
  1. Troche - dissolve 1 troche 5 times/day for 14 days
  2. Cream - apply twice daily
  3. Solution - rinse twice daily
26
Q

What is the adverse effect of clotrimazole

A

abnormal liver function

27
Q

Name the two topical antifungals

A
  1. nystatin (Mycostatin)

2. clotrimazole (Mycelex)

28
Q

Name the systemic antifungals

A

Azole antifungals

  • itraconazole (Sporanox)
  • fluconazole (Diflucan)
29
Q

Why do you avoid systemic anti fungal drugs

A
  1. Promotes resistance of fungal organisms
  2. Many dangerous drug interactions
  3. Hepatotoxic
  4. itraconazole = severe cardiovascular side effects; neuropathy
30
Q

T or F, Reserve systemic antifungal agents for severe cases

A

True

31
Q

Name the parenteral anti fungal drug

A

amphotericin

32
Q

How is amphotericin given?

A

by IV

33
Q

amphotericin is the most effective drug for what?

A

against deep-seated mycotic infections

- used for fungal infections associated with HIV

34
Q

Treatment for viral infections includes combination therapy of?

A

Antiviral drug
Topical anesthetics
Fluids, vitamins/minerals, rest

35
Q

Vesicular viral lesion =

A

Contagious

36
Q

Viral vesicle breaks =

A

Open lesion with draining fluid = contagious

37
Q

How long do viral lesions last?

A

10 days

38
Q

Are antibiotics effective for viral infections? Is anything else contraindicated?

A

No, they are ineffective

- Systemic corticosteroids are contraindicated for use during viral illnesses

39
Q

Mechanism of Acyclovir (Zovirax)

A

Inhibits viral DNA polymerase preferentially, inhibiting viral replication

40
Q

How is Acyclovir administered?

A

Systemically and topically
Systemic: recurrent mucosal and cutaneous herpes simplex infections
Topical: herpes labialis, mucocutaneous infections

41
Q

Dosage forms of acyclovir

A

oral
cream/ointment
suspension
injection

42
Q

2 different prescription examples for Herpes Simplex (primary infection)

A
  1. Zovirax 200 mg capsules
    Disp: 50 capsules
    Sig: Take 1 capsule 5 times/day for 10 days
  2. Zovirax 200 mg capsules
    Disp: 60 capsules
    Sign: Take 2 capsules 3 times/day for 10 days
43
Q

What is Xerese

A

Acyclovir 5% and hydrocoritsone 1%

External use only: lips and face

44
Q

What is Penciclovir (Denver)?

A

For Herpes labialis: apply only to lips and face

Effect not established in immunocompromised patients

45
Q

What is Famciclovir (Famvir) used for?

A

In immunocompetent patients

46
Q

Primary use for Valacyclovir (Valtrex)

A

genital herpes suppression therapy

47
Q

Side Effects of all antiviral drugs taken systemically

A 
Bone marrow suppression
Blood dispraises
-Thrombocytopenia
- Leukopenia
- Aplastic anemia

Pharmacology (24 decks)

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