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Pharmacology > ENT > Flashcards

ENT Flashcards

1
Q

What are the routes of transmucosal drug delivery

A 
Nasal
Rectal
Vaginal
Ocular
Oral cavity
 (Buccal, Sublingual, Local)
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2
Q

What is transmucosal administration?

A

Systemic absorption across mucosal linings.

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3
Q

What of the benefits of transmucosal drug delivery?

A

Avoids first-pass metabolism
Avoids enzymatic degradation within GI tract
Oral mucosa
Rich blood supply
Short recovery time after stress or damage
Cell turnover within 5 – 6 days
Tolerant to potential allergens

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4
Q

What patients should you avoid transmucosal drug delivery?

A

Pt w/ nausea

Careful stroke/facial paralysis

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5
Q

What benefits of sublingual delivery?

A

High drug concentrations in sublingual region before systemic absorption
Rapid onset of action

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6
Q

What population should you not use sublingual delivery

A

Smokers (vasoconstriction caused by smoking may decrease absorption)

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7
Q

What are the two categories of drugs that treat dizziness

A

Anticholinergics

Antihistamines

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8
Q

What are the symptoms of anticholinergic toxidrome?

A 
Hot as Hades - Fever
Fast as a Hare - Tachycardia
Dry as a Bone – Lack of diaphoresis
Red as a Beet – Flushed skin
Mad as a Hatter – Delirium
Full as a Tick – Urinary retention
Blind as a Bat – Mydriasis
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9
Q

What class of drugs is Scopolamine and what does it treat?

A

Drug class: Anticholinergic
Most effective medication for motion sickness
Transdermal preparation for motion sickness
Indicated for treatment of n/v assoc with motion sickness and post-op recovery
Applied to post auricular skin

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10
Q

How is scopolamine administered?

A

Commerical patch

Compounded gel or cream

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11
Q

Which barriers does scopolamine across?

A

Cross BBB

Cross placenta

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12
Q

What conditions is scopolamine contraindicated for?

A

Angle closure glaucoma

Oral: obstructive uropathy or GI disease

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13
Q

What is the warning for scopolamine?

A

Idiosyncratic psychoiss

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14
Q

What are the cautions for scopolamine?

A

Chronic open-angle glaucoma
Peds, Elderly (dose may be increased for these populations)
Driving motor vehicle or operating heavy machinery

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15
Q

How do you dose scopolamine?

A

Commerical patch

Compounded gel or cream

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16
Q

What dosing instructions should you give the patient for the scopolamine patch?

A

Patch behind the ear 4 hrs prior to the need for effect
One patch lasts 3 days
If patch falls off, add new patch behind other ear
Wash hands with soap and water after applying patch
Do not cut patch
Dose-dumping

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17
Q

What off label condition is scopolamine used for?

A

Vertigo

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18
Q

What are the 3 dosage forms in the oral cavity?

A

Buccal
Sublingual
Local

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19
Q

What receptors are involved in allergic reactions?

A

H1 receptor

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20
Q

Why does an epipen help with Type 1 allergic reactions w/anaphylaxis?

A

Functional antagonist to histamine

21
Q

Name was 1st generation competitive H1 receptor antagonists?

A 
Meclizine (Bonine, Antivert)
Hydroxyzine (Atarax)
Dimenhydrinate (Dramamine)
Diphenhydramine (Benadryl)
Promethazine (Phenergan)
Brompheniramine (Bromax)
Chlorpheniramine (Allergy Relief)
Doxylamine (Alka Seltzer Plus)
(Some may be inverse agonists)
22
Q

How do you dose the epipen?

A

IM injection anterolateral thigh

23
Q

What are the ADRs for epipen (epinephrine)

A

Anxiety, restlessness, tremor, weakness, palpitations, pallor, N/V, HA, respiratory issues

24
Q

Organize the oral mucosal permeability higher to lower.

A

sublingua l> buccal» palatal

25
Q

What are the disadvantages to sublingual administration?

A

Constant salivary action
Difficult for dosage forms to remain in place
Good for drugs with short delivery period and infrequent administration
Low drug permeability

26
Q

Where are buccal drugs administered?

A

Drug administration through mucus membranes lining the cheeks and area between gums and upper and lower lips to systemic circulation

27
Q

What are the advantages and disadvantages of buccal administration?

A

No water required
Rapid onset of action due to fast dissolution
lower bioavailability

28
Q

What does Scopolamine contain?

A

Henbane (belladonna)

29
Q

What is the MOA of Scopolamine?

A

Competitive antagonist at muscarinic receptors
Acts on smooth muscles that respond to acetylcholine but lack cholinergic innervation
blocks cholinergic transmission from vestibular nuclei to higher CNS centers and from the reticular formation to the vomiting center

30
Q

How does this present clinically?

A 
Inhibits saliva/sweat secretion 
decreases GI secretions and motility
decreases nausea/emesis
causes drowsiness
dilates pupils
increases heart rate
depresses motor function
31
Q

What is the absorption rate and half life of transdermal patches?

A

Absorption: Onset 4 hrs
Peak 24 hrs
t1/2 = 9.5 hrs

32
Q

What drugs are associated with direct histamine release?

A

Red-man’s syndrome
Opiods
Tubocurarine
Amphotercin

33
Q

What is the MOA of epinephrine?

A

Functional antagonist to histamine-induced bronchoconstriction
Alpha agonist
Decreases vasodilation and vascular permeability that leads to hypotension and loss of fluid volume
B2 agonist
Relaxes bronchial smooth muscle

34
Q

How do you properly dose the epipen?

A

IM injection anterolateral thigh
Glute may not give appropriate efficacy
(If accidentally injected in fingers, hands or feet, patient needs immediate medical attention)
(IV injection may cause cerebral hemorrhage)

35
Q

What are the ADRs for the epipen?

A

Anxiety, restlessness, tremor, weakness, palpitations, pallor, N/V, HA, respiratory issues
(Be careful when administering to CV pts. Epipen will cause tachycardia)

36
Q

What is the MOA for 1st gen antihistamines?

A

Block histamine H1 receptors:
Inhibits histamine effects on smooth muscle
Decreases inflammation, itching, sneezing, rhinorrhea, capillary permeability
Decreases CNS neurotransmitter release
Decreased cognitive and psychomotor performance
Increased sedation
Increased appetite

37
Q

What disadvantages of use a 1st gen antihistamine?

A

Distribute into all tissues, including CNS
Can also stimulate CNS causing central excitation, restlessness, nervousness and insomnia.
Non-selective
Significant anticholinergic effects
Dry mouth, urinary retention, sinus tachycardia
Alpha blocker effects
Hypotension, dizziness, reflex tachycardia
Serotonin blocker effects
Increased appetite

38
Q

What are the advantages of the 1st generation antihistamine?

A

Well-absorbed orally

High bioavailability

39
Q

What are the half lives for antihistamine?

A

Half-life = approx 4 – 6 hrs

Meclizine 12 – 24 hrs

40
Q

How long do the effects of antihistamines last?

A

Duration of effect: 4 – 6 hrs

(meclizine, diphenhydramine, chlorpheniramine) hydroxyzine 12 – 24 hrs

41
Q

What are the specific uses of some of the 1st generation antihistamines?

A

Promethazine used primarily as antiemetic
Hydroxyzine primarily for pruritus
Meclizine, dimenhydrinate for motion sickness

42
Q

Name the 2nd generation antihistamines.

A 
Loratadine (Claritin, Alavert)
Desloratadine (Clarinex)
Fexofenadine (Allegra)
Cetirizine (Zyrtec)
Levocetirizine (Xyzal) no advantage
43
Q

What are the benefits of using 2nd generation antihistamine over 1st generation.

A

Better side effect profile than 1st generation
Less sedating (Cetirizine, levocetirizine still have some sedation)
(Now 1st line for sneezing and itching due to allergic rhinitis)

44
Q

What are the indications for Fexofenadine (Allegra)?

A

Indications:
Treatment of allergic rhinitis in pts > 2 yo
Treatment of chronic urticaria in pts > 6 months

45
Q

What are the ADRs for Fexofenadine?

A

Headache, cough, URI, fever, back pain, dysmenorrhea

46
Q

What drugs interaction does Fexofenafine exhibit?

A

Ketoconazole, erythromycin, grapefruit juice, Al and Mg antacids (p450 issues)

47
Q

What are the indications for Cetirizine and Levocetirizine?

A

Allergic rhinitis in patients 6 months or older

Chronic urticaria in patients 6 months or older?

48
Q

What information should you consider before Cetirizine and Levocetirizine?

A 
Cmax in one hr
Crosses BBB so some sedation
Take w/ or w/o food
Half-life 8 -9 hrs
Prolonged in patients over 75yrs
Excreted via urine, some in feces
49
Q

What are ADRs for Cetirizine and Levocetirizine?

A

Somnolence, fatigue, dry mouth, dizziness, headache, abdominal pain, and nausea

Pharmacology (13 decks)

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