TRANS 063 EENT PHARMA

Question 1

Mydriatic vs Cycloplegic

Answer 1

• Mydriatic → induces dilation of pupils
• Cycloplegic → induces paralysis of ciliary muscle, resulting in
loss of accommodation
• Mostly anticholinergic agents

Question 2

Tropicamide, Atropine, Homatropine, Cyclopentolate

what drug class?

Answer 2

MYDRIATIC/ CYCLOPLEGIC AGENTS

Question 3

• Widely used to induce mydriasis to facilitate dilated
fundoscopy
• Blocks muscarinic M4 receptors on the iris sphincter muscle
and ciliary muscle, causing pupillary dilation and paralysis of
ciliary muscle

Answer 3

TROPICAMIDE

Question 4

Onset of action and duration of effect of tropicamide?

Answer 4

• Onset of action: 20-30 minutes
• Duration of effect: 4-6 hours
• AE: Stinging, irritation, blurred vision, dry mouth, headache,
increased IOP

Question 5

Most potent mydriatic with the longest duration of action (7
days)
• Used to dilate the pupil for dilated eye examinations
• Used to treat uveitis and iritis to immobilize the ciliary muscle
and prevent or break down adhesions
• AE: Stinging, irritation, blurred vision, dry mouth, headache,
increased IOP

Answer 5

Atropine

Question 6

• Inactive carbonic anhydrase and sodium pumps, decreasing aqueous humor production → decreased IOP
• AEs: Blurring of vision, bitter taste, dry eyes, irritation, headache

Answer 6

1. CARBONIC ANHYDRASE INHIBITORS (ACETAZOLAMIDE, BRINZOLAMIDE)

Question 7

• Considered first-line treatments for glaucoma
• Increase drainage of aqueous humor
• Once-daily dosing
• Notable AE: lengthening of eyelashes, increase in vellus hair, darkening of eyelid skin and iris color, puffy eye appearance

Sometimes used off label for lengthening the eyelashes

Answer 7

2. PROSTAGLANDIN ANALOGS

LATANOPROST, BIMATOPROST, TRAVOPROST

Question 8

• α2 effects → IOP reduction, neuroprotection (?)
• Decrease aqueous humor production and increases trabecular outflow
• AE: Dry mouth, tiredness, fatigue, blurred vision light sensitivity, tachyphylaxis (with apraclonidine)

Answer 8

3. ALPHA AGONISTS

APRACLONIDINE, BRIMONIDINE

Question 9

Block beta1 receptors in the ciliary epithelium, decreasing aqueous humor production
• AEs: Corneal epithelial erosions, corneal anesthesia

Answer 9

4. BETA AGONISTS

TIMOLOL

Question 10

Treatment/Management for corneal erosions, corneal abrasions?

Answer 10

Antibacterial. Takot tayo sa infection.

Question 11

Commonly used ocular antibiotics?

Answer 11

Usually quinolones. Ofloxacin, moxifloxacin, levofloxacin or yung ginagawang first-line tobramycin at si tobramycin with dexamethasone. Sikat na brand is Tobramycin (TOBREX) and si Tobramycin with Dexamethasone (TOBRADEX).

Question 12

Bakit may dexamethasone? Anti-inflammatory. Pero pag corneal abrasion hindi tayo gumagamit ng steroid. Plain lang na antimicrobial bakit kaya?

Answer 12

Kasi yung dexamethasone will prevent the normal healing process. Diba anti-inflammatory siya. Eh kailangan mo rin yung inflammatory, yung recruitment ng inflammatory cells para gumaling yung cornea.

Question 13

Kailan ka gagamit ng eye ointment kalian ka gagamit ng eye drops?

Answer 13

Eye ointment pag kailangan mo ng occlusion(?). Gusto mo yung medyo lubricating effect or you want an increased contact time between the corneal tissue and the medicine. Pero kung hindi naman important yung longer contact time pwede nang eye drops.

Question 14

• First-line treatment for many causes of ocular irritation, in particular for dry eye
• Topical eye drops or eye gels which are used in dry eye conditions (keratoconjunctivitis sicca/ dysfunctional tear syndrome)
 Some can be over-the-counter, some can only be procured by prescription.
 Gels and ointments are reserved for more severe cases kasi mas mahaba nga yung contact time sa cornea vs using ordinary eye drops.

Answer 14

B. OPHTHALMIC LUBRICANTS

• “Artificial tears”

Question 15

• Derivative of hyaluronic acid
• Humectant, lubricant and hypoosmotic
• Promotes corneal epithelial repair and controls localized inflammation

Answer 15

SODIUM HYALURONATE

Question 16

• Demulcent that forms protective layer over eyelid mucosa, relieve inflammation and irritation
• Demulcents: high-molecular weight polymers that mimic mucins and act to lubricate, protect and provide viscosity to eye drops
 Another common ingredient or common lubricant.

Answer 16

POLYTHYLENE GLYCOL (PEG)/ PROPYLENE GLYCOL

Question 17

• Hydrophilic polymers that coat and protect the eye
• Hydrogels that crosslink upon contact with the ocular surface to increase tear clearance times
• Must be mixed with other compounds because they are too viscous to instill alone onto the ocular surface
 Madalas niyo mae-encounter
 Similar to polyethylene glycol
 Madalas in combination

Answer 17

HYROXYMETHYLCELLULOSE, HYDROXYPROPYLCELLULOSE AND HYPROMELLOSE

Question 18

Common preservatives in artificial tears?

Answer 18

benzalkonium chloride

Question 19

Inhibits voltage-gated sodium channels on neuronal membranes, inhibiting action potential generation, nerve signal propagation and transmission
• Widely used in performing to provide anesthesia during the performance of ophthalmologic procedures

Answer 19

OCULAR ANESTHETIC: PROPARACAINE

Question 20

onset of action and duration of effect of proparacaine

Answer 20

• Onset of action: within 30 seconds

* Duration of effect: 10-15 minutes

Question 21

• H3 receptor antagonist
• Exact MOA is unknowm (increased cochlear blood flow)
• May have some benefit in reducing symptoms of vertigo and Meniere’s disease
• Genereally well-tolerated with low risk of adverse events
• Usual dose: 24-48 mg per day in 2-3 divided doses

Answer 21

1. BETAHISTINE

Question 22

Triad of Meniere’s disease:

Answer 22

hearing loss, tinnitus, vertigo

Question 23

• MOA: Inhibits vascular smooth muscle contractions by blocking L-type and T-type voltage-gated calcium channels
• Binds to dopamine D2 receptors, histamine H1 receptors and Ach receptors
• Used in the treatment of vertigo, Meniere’s disease, and motion sickness

Answer 23

CINNARIZINE

Question 24

o Lipophilic and cross the blood-brain barrier
o Have antimuscarinic effects
o Cause sedation because they are lipophilic. The more lipophilic drugs are, the easier they can cross the blood brain barrier, thereby, exhibiting the CNS adverse effects such as sedation.

Answer 24

Older first-generation agents of anti histamines

Question 25

What drug class? Cetirizine, Levocetirizine, Loratadine, Desloratadine, Ebastine, Bilastine

Answer 25

second generation anti histamine

Question 26

* Still commonly used over-the-counter drugs * May prevent and treat symptoms of allergic reactions and dry up nasal secretions but markedly causes sedation * Should not be used by persons who are driving or operating machinery

Answer 26

1. FIRST-GENERATION ANTIHISTAMINES | DIPHENHYDRAMINE, CHLORPHENAMINE, HYDROXYZINE

Question 27

may be used to suppress extrapyramidal side effects of first-generation antipsychotic drugs

Answer 27

• Diphenhydramine

Question 28

* Used mainly for the treatment of allergic rhinitis and chronic urtacrial * Provides the same efficacy as first-generation antihistamines but with little to nosedating effect

Answer 28

2. SECOND-GENERATION ANTIHISTAMINES | LORATADINE, CETIRIZINE, LEVOCETIRIZINE

Question 29

• MOA: Agonists of alpha adrenergic receptors → Vasoconstriction • Commonly used in patients where clogged nose is a problem  It reduces blood flow. Mas konti ang secretions kung mababa ang blood flow.

Answer 29

C. NASAL DECONGESTANTS Systemic: PHENYPROPANOLAMINE, PHENYLEPHRINE (tablet) Local: OXYMETAZOLINE (nasal spray)

Question 30

rebound congestion if used for a long period of time | o Pooling of secretions in patients with COPD

Answer 30

Oxymetazoline

Question 31

* Very effective for the treatment of allergic rhinitis with potent anti-inflammaotyr properties * Results in significant reduction in mediator and cytokine release along with a significant inhibition in the recruitment of basophils, eosinophils, neutrophils, and mononuclear cells to nasal secretions * Significantly improves quality of life and sleep of patient with allergic rhinitis * Superior to oral H1 antihistamines in controlling nasal sympotms, including nasdal congestion, with no significant difference in the relief of ocular sympyoms

Answer 31

INTRANASAL STEROIDS

Question 32

adverse effects of Budesonide and Beclomethasone

Answer 32

o Potential to suppress growth in children (particulary Budesonide and Beclomethasone; less likely with Mometasone furoate and Fluticasone propionate)

Question 33

• Commonly present as active ingredients of commercially-available moputhwashes or gargles • May provide soothing effects or temporary relief to symptoms of pharyngitis  Madalas ‘di ba nagrereseta ng pangmumog for symptomatic relief or adjunctive treatment. Let’s say for acute bacterial tonsillopharyngitis, the antibiotic of choice is amoxicillin. Kaya lang, it will not give symptomatic relief for difficulty of swallowing and pain kaya madalas nagbibigay ng other preparations. May soothing effect kasi or inherent antibacterial action.

Answer 33

E. ORAL ANTISEPTICS AND OTHER PREPARATIONS | CHLORHEXIDINE, HEXETIDINE

Question 34

• Broad-spectrum antimicrobial effective against gram-positive, gram-negative bacteria and fungi  Some say it also has antiviral properties pero ‘pag oral kasi di pa ganun ka-established. Mayroong hospital cleaning agents, hospital-grade disinfectants, na ito ang active ingredient. Iba syempre ‘yung preparation ng pharmacologic sa tao. • Positively-charged molecule that binds to the negatively-charged sites on the cell wall. It destabilizes the cell wall and interefere with osmosis. • Both bacteriostatic and bactericidal, depending on concentration

Answer 34

CHLORHEXIDINE GLUCONATE

Question 35

• Broad-spectrum antimicrobial effective against bacteria and fungi • Similar mechanism of action to chlorhexidine • Adverse effects: o Transient anesthesia – helps to the pain o Irritation o Sensitization o Taste disturbances

Answer 35

2. HEXETIDINE | Bactidol – brand name