Use LEFT and RIGHT arrow keys to navigate between flashcards;
Use UP and DOWN arrow keys to flip the card;
H to show hint;
A reads text to speech;
97 Cards in this Set
- Front
- Back
The important anti-inflammatory drugs are
|
corticosteroids
nsaids antihistamines decongestants mast cell stabalizes cyclosporin CNADMC MAD CNN |
|
The adrenal medulla secretes __________
while the cortex secretes |
medulla --> epi and norepi
cortex --> aldosterone, minerlocrotcoids, gucocorticoids --> supresses inflammation |
|
Anterior pituitary secretes _ which stimulates adrenal cortex
|
ACTH
|
|
the action of ________ is responsible for the production of cortisol
|
c-AMP
ACTH effects on adrenal cortex is also mediated by this |
|
Hypothalamus secretes __ which stimulates the anterior pit. to produce _____ which stimulates the release of _____ hormones
|
CRF
ACTH adrenal cortical |
|
Effects of glucocorticoids
|
increase production of glucose, glycogen storage increase
redistrubtion of body fat to back of neck and face (moon face) causes eupohria, insomnia, response of inflmmation are SUPRESSED |
|
the objective of making synthetic steriods has been to
|
enhance anti-inflammatory effects and reduce Na retention effects
|
|
T/F Prednisolone, dexamthason and fluorometholon significantly inhibit corneal reepithelialization
|
TRUE
also inhibits corneal adenylate cyclase activity |
|
Stroids may canse an increase in _______ in aqueous and vitreous humors and reduces _________
|
proteins and glucose increases
ascorbic acid decreases Aq outflow facility decreases leading to IOP increase!! |
|
T/F Steriods case opacities in lens to increase
|
T
|
|
T/F Steriods are used in ocular infection without worry
|
FALSE
steriods are contraindicated unless used in conjunction with anti-infective agents |
|
In general, steriods that are manufactured as _________ are more LIPID soluble and steriods that are manufcated as ____ are more water soluble
|
SUSPENSIONS
SOLUTIONS |
|
Which type of steriod is more water soluble?
|
solution
|
|
T/F ALCOHOL steriod solns are more LIPOHILIC than ACETATES
|
FALSE
Reverse is true |
|
T/F is epithelium is intact, acetate steroid form produces significantly higher corneal and aq steriod levels than phosphate derivates
|
TRUE
however, if epithelium is not inact, the drug level is higher for phosphate than acetate!!! |
|
Suspension steriods are better at treating _____- eye disease, and solutiosn are better for treating ________ eye diseases
|
INTERNAL
EXTERNAL |
|
T/F the naturalyl occuring steriod hydrocortisone has the most anti-inflammatory activity
|
FALSE
has the least |
|
6 synthetic steriod drugs
|
Prednisolone
Dexamethasone Fluromtholone Medrysone Loteprednol Rimexolone |
|
T/F Hydrocortisone is not avalable as a single entity drug
|
TRUE
must be mixed with various antbiotics |
|
The most effective anti-inflam topical ocular steriod for anterior segment ocular inflammation is
|
1% acetate prednisolone
|
|
The first drug of choice for treating moderate to severe forms of ocular inflammation
|
prenisolone
|
|
second drug of choice for treating moderate to severe forms of ocular inflammation
|
dexamethasone
|
|
This drug is a fluorinated structural analog of progesterone
|
flurometholone
|
|
The acetate form (suspension) of Flurometholone appears to be _______ effective than the alocohol form and as effective as ___ in its anterior seg anti-inflam properties
|
MORE
Prednisolone |
|
The alcohol form of Flurotheolone is the drug of choice for treating
|
LONG TERM chronic external ocular inflammation because it is less likely to elevate IOP than prednisolone and dexamthosone
|
|
The least likely available topical ocular steriod to cause increase in IOP is
|
medrysone.
It penetrates cornea VERY poorly. |
|
Loteprednol has little tendency to elevate IOP because
|
it immediately metabolizes to an inactive form once it reaches target tissue. VERY SAFE!
|
|
Loteprednol is avaible in
|
.5% and .2% suspension
lower concentration is approved for ocular allergies and higher is approved for anterior segment inflammation, it is just as efficacious as 1% prednisolone. |
|
This topical steroid is avalable as a dermatological cream
|
Triamcinolone. Useful in treating lid skin allergic reactions.
NOT to be used directly on eye. |
|
T/F long term high doses of ocular steriods should be reduced gradually
|
TRUE
|
|
These three ocular steriods are safest and shoudl be used whenever possible
|
prenisolone
fluormetholone medrysone |
|
For systemic administration of steriod drugs use
|
predniosne and triamcinolone and use minimal effective dose for shortest time possible
|
|
for local injections of steroid drugs, use
|
methylprednisolone acetate or triamcinolone
|
|
2 intraocular steroidal implants
|
dexamethasone mplant
flucinolone acetonide implant |
|
T/F Dexamethasone implant has a zero order kinetics with anti-inflam effects lasting days to weeks
|
T
implanted during caract surgery in anterior chamber |
|
Fluocinolne acetonide implant is used for
|
noninfectious posterior uveitis, can release drug for up to 3 years
|
|
Possible contraindications for steriods
|
diabetes mellitus, infections, chronic renal failure, ulcers, glaucoma
|
|
Drug interactions with steriods
|
rifampin, barbituates, anticoagulant drugs
|
|
ALTERNATE DAY THERAPY
|
Method not widely accepted
Used only for shorter acting systemic steroid such as prednisolone indicated Useful when long term therapy indicated |
|
ACTIONS OF NSAID
In ascending concentration of dose the following effects occur when these drugs are administered systemically |
Antiplatelet (reduced blood clotting)
Analgesic (reduction pain sensation) Antipyretic (reduced fever) Anti-inflammation |
|
Since NSAIDs inhibit cyclo-oxygenase but not lipooxygenase, these agents only inhibit ocular inflammation induced by prostaglandins but not _______________
|
leukotrienes
|
|
COX-1 produces prostaglandins that have _____________ such as _______ and ____________
|
cytoprotective effects
Mucus production and Mediation of platelet aggregation |
|
COX-2 produces prostaglandins that have ____________
In eye effects include the following: |
pro-inflammatory effects
post-op inflammation, uveitis, allergic conjunctivitis, miosis and cystoid macular edema (CME) |
|
T/F Cox-1 is proinflammatory
|
FALSE, that is cox-2
|
|
The lower the IC50 the ___________ the potency
|
HIGHER!!
|
|
IC50 FOR COX-1 in order from highest potency to lowest
|
Flurbiprofen
Ketorolac Nepafenac Bromfenac Diclofenac FKN BD |
|
IC50 FOR COX-2 in order of highest potency to lowest
|
Bromfenac
Diclofenac Flurbiprofen Ketorolac Nepafenac |
|
Topical NSAIDS include
|
Diclofenac sodium (Voltaren)
Keterolac (Acular) Flurbiprofen (Ocufen) Suprofen (Profenal) Nepafenac (Nevanac) Bromfenac (Xibrom) |
|
T/F DICLOFENAC SODIUM
(Voltaren, 0.1% sol.) is a topical NSAID that effects IOP levels |
FALSE
An acetic acid derivative that reduces pain and inflammation and has no significant effect on IOP –FDA approved indications: Tx of post op (cataract) ocular inflammation and corneal refractive surgery |
|
KETEROLAC
(Acular, 0.5% solution is a topical NSAID that is used for |
Relief of ocular itching due to seasonal allergy
Post-op cataract surgery inflammation |
|
FLURBIPROFEN is a topical NSAID that is used for
|
Blockade of intraoperative miosis, 1qtt q1/2 hr beginning 2 hrs prior to surgery
|
|
SUPROFEN
is a topical NSAID used for |
Intraoperative miosis, 2qtts qid day before surgery and 2 qtts 3, 2, and 1 hr before surgery
|
|
First FDA approved topical ocular non steroidal anti-inflammatory prodrug
|
NEPAFENAC
|
|
T/F Nepafenac is a topical nsaid that easily penetrates the cornea
|
T
|
|
Uses of Nepafenac, a topical nsaid
|
Treatment of inflammation and pain associated with cataract surgery –TID dosing starting one day prior to surgery and continuing 2 weeks post operative –As with all ocular suspension, the bottle must be shaken before drug administration
|
|
BROMFENAC is a _________ that is used to_________
|
topical NSAID
–Inhibits cyclooxygenase •FDA approved use –Treatment of inflammation and pain associated with cataract surgery |
|
T/F NSAIDs to not effect time of corneal healing
|
FALSE
they increase the time it takes the cornea to heal |
|
Type I (Immediate)hypersensitivity reaction definition
|
involves mast cells, antigens, antibodies and histamine –Allergic and vernal conjunctivitis
|
|
Type IV (Delayed)hypersensitivity reaction involves
|
involves T lymphocytes antigens and lymphokines –Vernal conjunctivitis, atopic keratoconjunctivitis & preservative induced blepharoconjunctivitis in CL wear
|
|
histamine is stored in these cells
|
mast
|
|
H1 receptors are found in
|
Smooth muscle of bronchi, blood vessels & intestines
|
|
H2 receptors are found in
|
Gastric parietal cells, heart, pulmonary blood vessels, cells of immune system, and other tissues
|
|
T/F
H1 ANTIHISTAMINES Reversibly bind to H1 receptors blocking histamine and inhibiting Type I reactions |
T
Also have antimuscarinic, local anesthetic and CNS properties (depression or stimula-tion) |
|
H1 ANTIHISTAMINES onset is ____ min, max effect in _____ hours and last _____ hours
|
•Onset 30 min., max. 1-2 hrs., duration 4-8 hrs.
|
|
H1 ANTIHISTAMINES are metabolized by _____ and excreted by _____
|
Metabolized by liver and excreted in urine
|
|
SINGLE-DRUG TOPICAL OCULAR ANTIHISTAMINES
|
1.Levocabastine
2.Emadastine difumarate (Emadine) |
|
ANTIHISTAMINE-VASOCONSTRICTOR COMBINATIONS
|
•Antazoline-naphazoline (Albalon-A) •Pheniramine-naphazoline (Opcon-A)
•Pyrilamine-phenylephrine (Prefrin-A) •Pheniramine-phenylephine (AK-Vernacon) |
|
Diphenhydramine (Benedryl) is a ____ H1 receptor ______ type
|
Sedating H1 receptor competitive antagonist type
|
|
•Non-sedating H1 receptor non-competitive antagonist types include
|
Chlorpheniramine (Chlor-trimeton)
Loratadine (Claritin), Desloratadine (Clarinex), Fexofenadine (Allegra) and Cetirizine (Zyrtec) |
|
What causes benedryl to be sedating?
|
Lipid solubility allows entrance into brain with resulting sedation
|
|
T/F DIPHENHYDRAMINE
(Benedryl)Has antimusarinic effects |
FALSE
anticholinergic |
|
Decongestants are _____ agonists that _______ conjunctival vessels
|
Adrenergic agonists
•Constrict conjunctival vessels |
|
This warning primarily applies to systemically administered decongestants
|
•Discontinue use prior to use of inhalation type general anesthetics (cyclopropane & halothane) which sensitize myocardium to sympathomimetics
|
|
MAST CELL STABILIZERS
|
•CROMOLYN SODIUM
•NEDROCROMIL SODIUM (Alocril, Allergan) •LODOXAMIDE (Alomide, Alcon) •PERMIROLAST POTASSIUM CNLP |
|
T/F Chromoyln Sodium is a mast cell stabalize that gives immediate relief of ACTUE allergic symptoms
|
FALSE
Does not give immediate relief of acute allergic symptoms but very useful for management of chronic allergies Type I allergic conjunctivitis: relief of symptoms of acute disease occurs within 7 days •Indicated for relief of chronic allergies –Vernal conjunctivitis: Used with steroids –Giant papillary conjunctivitis |
|
H1 receptors are found in
|
Smooth muscle of bronchi, blood vessels & intestines
|
|
H2 receptors are found in
|
Gastric parietal cells, heart, pulmonary blood vessels, cells of immune system, and other tissues
|
|
T/F
H1 ANTIHISTAMINES Reversibly bind to H1 receptors blocking histamine and inhibiting Type I reactions |
T
Also have antimuscarinic, local anesthetic and CNS properties (depression or stimula-tion) |
|
H1 ANTIHISTAMINES onset is ____ min, max effect in _____ hours and last _____ hours
|
•Onset 30 min., max. 1-2 hrs., duration 4-8 hrs.
|
|
H1 ANTIHISTAMINES are metabolized by _____ and excreted by _____
|
Metabolized by liver and excreted in urine
|
|
SINGLE-DRUG TOPICAL OCULAR ANTIHISTAMINES
|
1.Levocabastine
2.Emadastine difumarate (Emadine) |
|
ANTIHISTAMINE-VASOCONSTRICTOR COMBINATIONS
|
•Antazoline-naphazoline (Albalon-A) •Pheniramine-naphazoline (Opcon-A)
•Pyrilamine-phenylephrine (Prefrin-A) •Pheniramine-phenylephine (AK-Vernacon) |
|
Diphenhydramine (Benedryl) is a ____ H1 receptor ______ type
|
Sedating H1 receptor competitive antagonist type
|
|
•Non-sedating H1 receptor non-competitive antagonist types include
|
Chlorpheniramine (Chlor-trimeton)
Loratadine (Claritin), Desloratadine (Clarinex), Fexofenadine (Allegra) and Cetirizine (Zyrtec) |
|
What causes benedryl to be sedating?
|
Lipid solubility allows entrance into brain with resulting sedation
|
|
T/F DIPHENHYDRAMINE
(Benedryl)Has antimusarinic effects |
FALSE
anticholinergic |
|
Decongestants are _____ agonists that _______ conjunctival vessels
|
Adrenergic agonists
•Constrict conjunctival vessels |
|
This warning primarily applies to systemically administered decongestants
|
•Discontinue use prior to use of inhalation type general anesthetics (cyclopropane & halothane) which sensitize myocardium to sympathomimetics
|
|
MAST CELL STABILIZERS
|
•CROMOLYN SODIUM
•NEDROCROMIL SODIUM (Alocril, Allergan) •LODOXAMIDE (Alomide, Alcon) •PERMIROLAST POTASSIUM CNLP |
|
T/F Chromoyln Sodium is a mast cell stabalize that gives immediate relief of ACTUE allergic symptoms
|
FALSE
Does not give immediate relief of acute allergic symptoms but very useful for management of chronic allergies Type I allergic conjunctivitis: relief of symptoms of acute disease occurs within 7 days •Indicated for relief of chronic allergies –Vernal conjunctivitis: Used with steroids –Giant papillary conjunctivitis |
|
This mast cell stabalizer not only inhibits histamine release, but also inhibits chemotaxis of eosinophils and release of pro-inflammatory substances from these cells
|
NEDROCROMIL
|
|
Clinical uses of nedrocromil (a mast cell stabalizer)
|
Perennial allergic conjunctivitis and GPC
|
|
COMBINATION ANTIHISTAMINE-MAST CELLS include
|
STABILIZERSOLOPATADINE (Pataday, Alcon)
OLOPATADINE (Patanol, Alcon) KETOTIFEN FUMARATE (Zaditor, Ciba) AZELASTINE HCL (Optivar, B&L) EPINASTINE HCL (Elastat, Allergan) A-OK'ES |
|
T/F Pataday should not administer while CL in eye since preservative (Benz. Cl) absorbs into Cl
|
T
|
|
_________ is an immunomodulator with anti-inflammatory effects, but exact mechanism not known
|
CYCLOSPORIN
(Restasis) |
|
Restasis is used clinically in patients with
|
keratoconjunctivitis sicca secondary to reduced tear production due to ocular inflammation, Restasis is believed to act as a partial immunomodulator
•Results in increased tear production |
|
Dosage and Administration of Restasis includes
|
–1qtt q12h
- Shake bottle –Can be used concurrently with artificial tears |