Systemic Pharm Flashcards
What are three targets of natimicrobials
Cell wall
DNA
Proteins
What parts of the cell wall in microbes do we target
Peptidoglyan (brick)
Transpeptidase (glue)
Cell wall synthesis blockers
Bacitracin
PNC
Cephalosporins
PCNs
Amoxicillin
Dicloxicilin
Cephalosporins
Cephalexin
Ceftriaxone
Protein synthesis inhibitors target
30s and 50s ribosomal subunits
30s protein synthesis inhibitors
buy AT 30 Aminoglycosides -gentamicin -tobramycin Tetracyclines -tetracycline -doxycline -minocycline
50s protein synthesis inhibitors
Collect Money at 50
- macrolides: erythromycin, azithromycin, alrithromycin
- Clindamycin (lincomycin)
- Chloramphenacol
How do we inhibit DNA for microbes
Folic acid synthesis (synthase and reductase)
DNA gyrase and topopolymerase 4 (FQs)
Inhibitors of folate synthase
Sulfonamide
Trimethoprim
Pyrimethamine
DNA gyrase and topoisomerase inhibitors
FQs
- 2nd G=ciprofloxain, ofloxacin
- 3rd G=levofloxacin
- 4th G=gatifloxacin, moxifloxicin, besifloxacin
Peptidoglycan
The structural building block of bacterial cell walls; it contains polysaccharide chains that are cross linked via the enzyme transpeptidase. Bacitracin inhibits the transfer of peptidoglycan into the growing bacterial cell wall. All PCNs and cephalopods inhibit cell wall synthesis by inhibiting transpeptidase
MOA of bacitracin
Prevents bacterial cell wall synthesis by inhibiting the transfer of peptidoglycans
Clinical indications of bacitracin
Bacterial agent that is only effectsi against gram +; only available in ointment form and is often RXed for the treatment of blepharitis (staph)
Polysporin
Broads spectrum topical ophthalmic antibiotic ointment that contains the gram + coverage of bacitracin with the gram - coverage of polymyxin B
Neosporin
Neomycin + polysporin
Polysporin=bacitracin + polymyxinB
MOA of PCN (amoxicillin and dicloxacillin)
Inhibits transpeptidase
Which has better gram - coverage, amoxicillin or dicloxacillin
Amoxicillin
Penicillinase
Amoxicillin is not resistance to this but dicloxacillin is
Amoxicillin + calvulonic acid=Augmentin and this IS resistant to penicillinase
Dicloxacillin and augmentin are RXed for
Combat bacterial infections of the eyelid (hordeolum, preseptal cellulitis) caused by S aureus
DOC for MSS
Dicloxacillin
Not effective against MRSA though
Adverse effects of PCN
Hypersensitivity reaction
- type 1=anaphylactic shock and urticaria
- type 4=contact dermatitis
Render oral BC ineffective
Can cause SJS
Generally PCNs are very safe in all trimesters of pregnancy
MOA of cephalosporins (cephalexin, Ceftriaxone)
Inhibit transpeptidase
Clinical indications of cephalosporins
Similar to PCNs, all have good gram + coverage. 3rd and 4th generation are more effective against gram negative
Cephalexin uses
1st generation cephalosporin
Skin infections (that are primarily caused by gram + bacteria)
Dacryoadenitis, dacryocystitis, and preseptal cellulitis
Ceftriaxone
3rd generation cephalosporin
Gonorrhea
IV is treatment of choice for gonococcal conjunctivitis and orbital cellulitis
Treatment of choice for gonococcal conjunctivitis and orbital cellulitis
IV ceftriaxone
Gram negative
Adverse effects of cephalosporins
Hypersensitivity reactions
Alters vit K absorption, thinning of hte blood
Contraindicated in warfarin
Coverage cephalosporin
1st generation=gram +
3rd and 4th generation gram + and -
Which has better gram negative coverage, aminoglycosides or tetracyclines
Aminoglycosides
Aminoglycosides
Gentamicin
Tobramycin
MOA of aminoglycosides (tobramycin/gentamicin)
Bind to the 30s subunit of the bacterial ribosome to inhibit bacterial protein synthesis; effective against gram negative and gram + bacteria, with better coverage of the gram negative spectrum
Ocular indications of aminoglycosides (tobramycin/gentamicin)
Tobramycin is available in topical ophthalmic form and ointment form. Gentamicin and tobramycin topical ophthalmic solutions are available in fortified concentration, and are RXed with fortified cefazolin for the treatment of sight threatening ulcers
Tobradex
Tobramycin + dexamethasone
Inflammatory ocular conditions with an associated bacterial infection (staph marginal keratitis, corneal infiltrates)
AmiNOglycOSides
Nephtotoxicity
Ototoxicity
Ocular surface disease
Drugs taken on an empty stomach
PAT
PCNs, azithromycin, tetras
*doxy is the exception
Adverse effects of aminoglycosides
Topical ophthalmic aminoglycosides cause SPK and delayed healing
Tetracyclines
30s
Tetracycline
Doxycycline
Minocycline
MOA of tetracycline
Inhibit bacterial protein synthesis by binding to the 30s ribosomal subunit and preventing access to aminoacyl tRNA; they are bacteriostatic ABx
Clinical inidincations of doxycycline
Meibomianitis
Acne rosacea
Chlamydia ocular infections
Post RCE
TAKEN WITH FOOD
Minocyline indications
Low doses for long term managment of acne vulgaris
Pharmacokinetics of tetracyclines
The absorption in the GI tract is impaired by cations in dairy products, antacids, and iron-containing compounds. The primary route of excretion of through the kidney; thus tetras are contraindicated in pateitns with renal failure. Doxy is th excretion, it can be taken with food and is eliminated in fecal matter, and can therefore be RXed in patients with renal failure
Adverse affects of tetras
Contraindicated in pregnancy and in children. Side effects include pseudotumor cerebri, bone growth retardation, and discoloring of teeth. Minocyline may cause blue sclera and pigmented cysts on the conjunctiva
Blockers of the 50s ribosomal subunit
CM
Chloramphenicol, clindamycin,lincomycin, marolides (erythromycin, azithromycin, clarithromycin)
Chloramphenicol MOA
Inhibits bacterial protein synthesis by binding to the 50S ribosomal subunit; it is effective against gram + and gram - bacteria. It can be formulated as an ointment for topical ophthalmic solution
Dinosaur
We dont use it that much anymore
Drugs contraindicated in pregnancy
FAT
FQs
Aminoglycosides
Tetras
Drugs that are safe in pregnancy
PAC
Pens
Azithromycin
Cephalosporin
P cerebri drugs
CATS Contraceptive Acutane Tetra Synthroid/steroid
Drugs that can cause a blue scleral
Steroids
Minocycline
Adver effects of chloramphenicol
TOPICAL ophthalmic use has caused fatal aplastic anemia
Extended therapy may result in optic neuritis
What is the only topical drug that can cause fatal aplastic anemia
Chloramphenicol
MOA of macrolides (erythromycin, azithromycin, clarithromycin)
Inhibit the bacterial protein synthesis by binding to the 50S subunit of the bacterial ribosome
What can treat chlamydia
Doxy
Azithromycin
Uses of oral azithromycin
Chlamydia infections (trachoma and AIC) Single gram dose Taken on an empty stomach
Topical ophthalmic azithromycin uses
Bacterial conjunctivitis and blepharitis
BID x 2 days, then QD x 5 days
Topical ophthalmic erythromycin ointment uses
Uncommonly RXed for active bacterial infections due to its poor resistance profile; it is more commonly RXed for prophylaxis and is dosed at night. It is also RXed for prophylaxis of gonococcal ophthalmia neonatorum
Oral clarithromycin uses
Respiratory infections
Azasite
Contains the preservative BAK. Patients who wear CL are advised against CL wear during the treatment with azasite
MOA of lincomycin/clindamycin
Inhibit the bacterial protein synthesis by REVERSIBLY binding to the 50s subunit of the bacterial ribosome
Clinical indications of clindamycin/lincomycin
MRSA
Drugs for MRSA
Bacteria Can’t Decide
Bactrim (TMP-sulf)
Clindamycin
Doxycycline
Sulfonamide MOA
Inhibit dihydropteroate synthase, an enzyme that converts PABA to dihydrofolic acid as the first step of folic acid synthesis; these drugs are bacteriostatic agents that are RXed to treat gram + and gram - infections
Ophthalmic indications of sulfonamide
Rarely used topically
Side effects of topical sulfonamide
Burning, stinging, contact dermatitis, and local photosensitization
Systemic indications of sulfonamide
Sulfadiazine + pyrimethamine=toxo treatment
Sulfamethoxazole + trimethorpim=bactrim
Adverse effects of sulfonamides
Can cause kernicterus in infants due to bilirubin accumulation within the brain (they are contraindicated during pregnancy); they may also have a myopic shift in the patients refractive error. Topical and oral sulfonamides may also cause SJS
Trimethoprim and pyrimethamine MOA
Inhibit dihycrofolate reductase, an enzyme that converts dihydrofolic acid to tetrahydrofolic acid in the second step of folic acid synthesis
Trim reduces
Clinical indications of trimethoprim
Gram +/-, not as effective against pseudomonas
Combo with polymyxin B as polytrim
Indications of pyrimethamine
Given orally with sulfadi for toxoplasmosis
What is the best to use for bacterial conjunctivits in kids
Polytrim
Most potent ophthalmic ABX against MRSA
Trimethoprim and tobramycin
Besifoxacin and vancomycin also
Adverse effects of trimethoprim/pyrimethamine
Oral trimethoprim can cause bone marrow suppression, resulting in aplastic anemia, leukopenia, and granulocytopenia, pyrmethamine can have similar toxicity
MOA of FQs
Rapidly inhibit bacterial DNA synthesis by inhibiting DNA gyrase and topoisomerase 4
2nd generation FQ
Cirpofloxacin
Ofloxacin
3rd generation FQs
Levofloxacin
4th generation FQs
Gatifloxacin
Moxifloxacin
Besifloxacin
Topical ophthalmic indications of FQs
Contact lens realted ulcers, corneal abrasions, and bacterial conjunctivitis
Systemic indications of FQs
Ciprofloxacin is RXed for gram - urinary and GI infections. Moxifloxacin is approved for the treatment of pneumonia, sinusitis, and intracranial-abdominal and skin infections
Adverse effects of FQs
ORAL fluroquinoLONES can hurt the attachment to your BONEs; causing tendinitis. Oral FQs are contraindicated in pregnancy, chidlren, and adolescents below the age of 18 due to damage in cartilage formation and inhibition of bone growth
Effectiveness of the differnt generations of FQs
There are 4 generations, 3 and 4 have been formulated with improved effectiveness against gram + infections, however these drugs continue to be potent against gram - bac as well
Topical FQs and kids
All of the TOPICAL (NEVER ORAL) FQs are approved for kids 1 year and older EXCEPT LEVOFLOXACIN
Bacteriostatic agents
Tetracyclines, trimethoprim, sulfacetamde, and to some degree, erythromycin
Bacteriocidal agents
PNS, Cephs, bacitracin, aminoglycosides, FQs
Number one symptom of TB
Night sweats
TB is caused by
Mycobacterium TB
Active TB
Treated with a combo therapy
Latent TB
Treated with isoniazid or rifampin monotherapy
Active TB treatment is
RIPE
- rifampin
- isoniazid
- ethambutol
Don’t need to know the P one
TB=RIPE Cheese
RIPE for the drugs
Cheese=caseous necrosis
MOA of rifampin
Prevents mRNA synthesis (transcription) by binding to the beta subunit of DNA dependent RNA POLYMERASE
Adverse effects of rifampin
Hepatotxicity (increased AST and ALT), orange/pink colored tears and urine
Isoniazid MOA
Prevents cell wall synthesis by inhibiting mycolic acid synthesis
Adverse effects of isoniazid
Hepatotoxicity, can also cause pyridoxine (vit B6) deficiency that may result in peripheral neuropathy. Rarely It can cause optic neuritis and optic atrophy, resulting in loss of vision
Ethambutol MOA
Inhibits synthesis of mycobacterium cell wall by inhibiting arabinosyl transferase
What are the two drugs that can be used in isolation for TB monotherapy (latent)
Rifampin
Isoniazid
Adverse effects of ethambutol
Optic neuritis (retrobulbar) May be reversible vision loss
What TB drug is known to cause retrobulbar optic neuritis
Ethambutol
Antivirals for the flu
Oseltamivir (tamiflu)
-inhibits influenza A and B viral neuraminidase
Conjunctivitis due to influenza in 1% pts has been reported
MOA of HIV therapy (Zidovudine [Retrovir])
Reverse transcriptase inhibitor
AIDs occurs at what CD 4 count
<200
Clinical indications of zidovudine (Retrovir)
Major component of three-drug therapy for HIV. Also used during pregnancy to lower the risk of transmitting HIV to the fetus (vertical transmission)
Adverse effects of zidovudine (Retrovir)
- Bone marrow suppression
- Lactic acidosis
- Muscle breakdown
Amblyopia and macular edema have also been reported
There is a vax for which Heps
A and B
None for C
Hepatitis C therapy
C=chronic
Ribavirin + interferon
MOA of ribivirin
Inhibits viral RNA polymerase
Always in combo with interferon for the treatment of hep C
Adverse effects of ribavirin
Conjunctivis
Retinopathy
Retinal vascular Occlusions
Ocular side effects of ribavirin
RIBAViriN RD Ischemia Bleeding Arterial and Venous occlusions Optic Neuritis
VA normally OK
Why kind of virus is herpes
DNA
What do all herpes meds do
Inhibit DNA polymerase
Trifluridine MOA
Inhibits DNA polymerase for the treatment of herpes simplex keratitis
Not used often because 9x day dosing and thimerosol
Acyclovir, valacyclovir, famcyclovir MOA
DNA polymerase inhibitors
Indications of acyclovir, valacyclovir, and famcyclovir
Cold sores, genital sores, and shingles. They may also be RXed for HZO, HSV keratitis, and prophylaxis against recurrent HSV keratitis
Adverse effects of acyclovir, valacyclovir, and famcyclovir
Headaches and GI effects
Renal dysfunction
-be careful in those with renal dysfunction and the elderly. Monitor closely
Oral antivirals
Used to treat HSV epithelial keratitis, but topical ophthalmic treatment is considered the standard of care. Oral dosages should be decreased in patients with kidney disease
Gancylovir
- DNA polymerase inhibitor
- reduced corneal toxicity, 5x/day dosing (better than viroptic)
- BAK instead of thimerosol
Clinical indications for gancyclovir
HSV keratitis
Intraocular sustained-release capsule for the treatment of CMV retinitis
CMV
Opportunistic infection
Vision threatening retinopathy in those with AIDS
-most common intraocualr infection in patients with AIDs
-treat with Zirgan (gancyclovir), if that doesnt work, use your safety “net” Foscarnet
Foscarnet
- SAfety net for CMV if gancyclovir fails
- DNA polymerase inhibitor, IV
- nehprotoxicity and seizures
Fungal ucler
Feathery edges
Immunocompromised
Chronic beat up cornea
Tree branch
Fungus: ergosterol
Component of fungal cell membranes that is not found in human or animal cell walls.
Antifungal drugs
Natamycin, amphotericin B, nystatin
Ketoconazole, fluconazole, and miconozole
Griseofulvin
MOA of natamycin, amphotericin B, and nystatin
Bind to ergosterol and form pores
Clinical indictions for natamycin
Approved for the treatment of fungal blepharitis, conjunctivits, and keratitis caused by susceptible organisms of Candida, Aspergillus, and Fusarium
Clinical indications for Amphotericin B
Broad spectrum antifungal.
Fungal keratitis, and IV form to treat systemic and intraocular fungal infections.
Nephrotoxicity is common in IV form
Clinical indications of Nystatin
Candida oral (thrush) and vaginal (yeast) infections Not indicated for ophthalmic use
MOA of ketoconazole, fluconazole, and miconazole
Inhibit ergosterol synthesis
Clinical indications of ketoconazole
First oral azole antifungal drug and is indicated for the treatment of severe fungal corneal ulcers, systemic fungal infections, and acanthoemeba
Indications of fluconazole
Orally, topically, or through subconjunctival injections
Adverse effects of the azoles
Hepatotoxicity
MOA of griseofulvin
Inhibits fungal mitosis by interfering with microtubule formation
Clinical indictions of griseofulvin
Scalp and skin, fingernails and toenails
Treatment of toxoplasmosis
Sulfadi + pyrimethamine
Antiparasitic drugs
Chloroquine
Lindane
MOA of chloroquine
- Results in the build up of heme within the RBCs; this accumulation is toxic to the “intra-erythrocytic” plasmodium parasite responsible for malaria
- Inhibits phosphlipase A2 to decrease inflammation, not generally used for this
Adverse effects of chloroquine
Whorl K
Bulls eye maculopathy: granular hyperpigmentation surrounded by zone of depigmentation
Binds melanin=migration of RPE cells-permanent
What does a plaquenil screening consist of
10-2 VF
SD-OCT
Why does chloroquine cause bulls eye maculopathy
Binds to melanin of the RPE cells, causing localized RPE damage and subsequent migration of RPE cells to the outer nuclear and OPL. The initial sign of bulls eye maculopathy is RPE mottling within the macula
Risk of developing bulls eye maculopathy in chloroquine
- > 2.3mg/kg body weight (Hydroxychloroquine is >5mg/kg)
- treatment > 5 years
- abnormal renal function
- high body fat
- > 60yo
- liver disease
- concomitant retinal disease
Scotomas of chloroquine
Central and paracentral most common
Lindane
Antiparacytic MOA: lipophlic structure absorbed through the exoskeleton of insects, resulting in seizures and death -lice, scabies -causes conjunctivits -not for the eyes
Peptidoglycan
The structural building block of bacterial cell walls; it contains polysaccharide chains that are cross linked via the enzyme transpeptidase. Bacitracin inhibits the transfer of peptidoglycan into the growing bacterial cell wall. All PCNs and cephalopods inhibit cell wall synthesis by inhibiting transpeptidase
MOA of bacitracin
Prevents bacterial cell wall synthesis by inhibiting the transfer of peptidoglycans
Clinical indications of bacitracin
Bacterial agent that is only effectsi against gram +; only available in ointment form and is often RXed for the treatment of blepharitis (staph)
Polysporin
Broads spectrum topical ophthalmic antibiotic ointment that contains the gram + coverage of bacitracin with the gram - coverage of polymyxin B
Neosporin
Neomycin + polysporin
Polysporin=bacitracin + polymyxinB
MOA of PCN (amoxicillin and dicloxacillin)
Inhibits transpeptidase
Which has better gram - coverage, amoxicillin or dicloxacillin
Amoxicillin
Penicillinase
Amoxicillin is not resistance to this but dicloxacillin is
Amoxicillin + calvulonic acid=Augmentin and this IS resistant to penicillinase
Dicloxacillin and augmentin are RXed for
Combat bacterial infections of the eyelid (hordeolum, preseptal cellulitis) caused by S aureus
DOC for MSS
Dicloxacillin
Not effective against MRSA though
Adverse effects of PCN
Hypersensitivity reaction
- type 1=anaphylactic shock and urticaria
- type 4=contact dermatitis
Render oral BC ineffective
Can cause SJS
Generally PCNs are very safe in all trimesters of pregnancy
MOA of cephalosporins (cephalexin, Ceftriaxone)
Inhibit transpeptidase
Clinical indications of cephalosporins
Similar to PCNs, all have good gram + coverage. 3rd and 4th generation are more effective against gram negative
Cephalexin uses
1st generation cephalosporin
Skin infections (that are primarily caused by gram + bacteria)
Dacryoadenitis, dacryocystitis, and preseptal cellulitis
Ceftriaxone
3rd generation cephalosporin
Gonorrhea
IV is treatment of choice for gonococcal conjunctivitis and orbital cellulitis
Treatment of choice for gonococcal conjunctivitis and orbital cellulitis
IV ceftriaxone
Gram negative
Adverse effects of cephalosporins
Hypersensitivity reactions
Alters vit K absorption, thinning of hte blood
Contraindicated in warfarin
Coverage cephalosporin
1st generation=gram +
3rd and 4th generation gram + and -
Which has better gram negative coverage, aminoglycosides or tetracyclines
Aminoglycosides
Aminoglycosides
Gentamicin
Tobramycin
MOA of aminoglycosides (tobramycin/gentamicin)
Bind to the 30s subunit of the bacterial ribosome to inhibit bacterial protein synthesis; effective against gram negative and gram + bacteria, with better coverage of the gram negative spectrum
Ocular indications of aminoglycosides (tobramycin/gentamicin)
Tobramycin is available in topical ophthalmic form and ointment form. Gentamicin and tobramycin topical ophthalmic solutions are available in fortified concentration, and are RXed with fortified cefazolin for the treatment of sight threatening ulcers
Tobradex
Tobramycin + dexamethasone
Inflammatory ocular conditions with an associated bacterial infection (staph marginal keratitis, corneal infiltrates)
AmiNOglycOSides
Nephtotoxicity
Ototoxicity
Ocular surface disease
Drugs taken on an empty stomach
PAT
PCNs, azithromycin, tetras
*doxy is the exception
Adverse effects of aminoglycosides
Topical ophthalmic aminoglycosides cause SPK and delayed healing
Tetracyclines
30s
Tetracycline
Doxycycline
Minocycline
MOA of tetracycline
Inhibit bacterial protein synthesis by binding to the 30s ribosomal subunit and preventing access to aminoacyl tRNA; they are bacteriostatic ABx
Clinical inidincations of doxycycline
Meibomianitis
Acne rosacea
Chlamydia ocular infections
Post RCE
TAKEN WITH FOOD
Minocyline indications
Low doses for long term managment of acne vulgaris
Pharmacokinetics of tetracyclines
The absorption in the GI tract is impaired by cations in dairy products, antacids, and iron-containing compounds. The primary route of excretion of through the kidney; thus tetras are contraindicated in pateitns with renal failure. Doxy is th excretion, it can be taken with food and is eliminated in fecal matter, and can therefore be RXed in patients with renal failure
Adverse affects of tetras
Contraindicated in pregnancy and in children. Side effects include pseudotumor cerebri, bone growth retardation, and discoloring of teeth. Minocyline may cause blue sclera and pigmented cysts on the conjunctiva
Blockers of the 50s ribosomal subunit
CM
Chloramphenicol, clindamycin,lincomycin, marolides (erythromycin, azithromycin, clarithromycin)
Chloramphenicol MOA
Inhibits bacterial protein synthesis by binding to the 50S ribosomal subunit; it is effective against gram + and gram - bacteria. It can be formulated as an ointment for topical ophthalmic solution
Dinosaur
We dont use it that much anymore
Drugs contraindicated in pregnancy
FAT
FQs
Aminoglycosides
Tetras
Drugs that are safe in pregnancy
PAC
Pens
Azithromycin
Cephalosporin
P cerebri drugs
CATS Contraceptive Acutane Tetra Synthroid/steroid
Drugs that can cause a blue scleral
Steroids
Minocycline
Adver effects of chloramphenicol
TOPICAL ophthalmic use has caused fatal aplastic anemia
Extended therapy may result in optic neuritis
What is the only topical drug that can cause fatal aplastic anemia
Chloramphenicol
MOA of macrolides (erythromycin, azithromycin, clarithromycin)
Inhibit the bacterial protein synthesis by binding to the 50S subunit of the bacterial ribosome
What can treat chlamydia
Doxy
Azithromycin
Uses of oral azithromycin
Chlamydia infections (trachoma and AIC) Single gram dose Taken on an empty stomach
Topical ophthalmic azithromycin uses
Bacterial conjunctivitis and blepharitis
BID x 2 days, then QD x 5 days
Topical ophthalmic erythromycin ointment uses
Uncommonly RXed for active bacterial infections due to its poor resistance profile; it is more commonly RXed for prophylaxis and is dosed at night. It is also RXed for prophylaxis of gonococcal ophthalmia neonatorum
Oral clarithromycin uses
Respiratory infections
Azasite
Contains the preservative BAK. Patients who wear CL are advised against CL wear during the treatment with azasite
MOA of lincomycin/clindamycin
Inhibit the bacterial protein synthesis by REVERSIBLY binding to the 50s subunit of the bacterial ribosome
Clinical indications of clindamycin/lincomycin
MRSA
Drugs for MRSA
Bacteria Can’t Decide
Bactrim (TMP-sulf)
Clindamycin
Doxycycline
Sulfonamide MOA
Inhibit dihydropteroate synthase, an enzyme that converts PABA to dihydrofolic acid as the first step of folic acid synthesis; these drugs are bacteriostatic agents that are RXed to treat gram + and gram - infections
Ophthalmic indications of sulfonamide
Rarely used topically
Side effects of topical sulfonamide
Burning, stinging, contact dermatitis, and local photosensitization
Systemic indications of sulfonamide
Sulfadiazine + pyrimethamine=toxo treatment
Sulfamethoxazole + trimethorpim=bactrim
Adverse effects of sulfonamides
Can cause kernicterus in infants due to bilirubin accumulation within the brain (they are contraindicated during pregnancy); they may also have a myopic shift in the patients refractive error. Topical and oral sulfonamides may also cause SJS
Trimethoprim and pyrimethamine MOA
Inhibit dihycrofolate reductase, an enzyme that converts dihydrofolic acid to tetrahydrofolic acid in the second step of folic acid synthesis
Trim reduces
Clinical indications of trimethoprim
Gram +/-, not as effective against pseudomonas
Combo with polymyxin B as polytrim
Indications of pyrimethamine
Given orally with sulfadi for toxoplasmosis
What is the best to use for bacterial conjunctivits in kids
Polytrim
Most potent ophthalmic ABX against MRSA
Trimethoprim and tobramycin
Besifoxacin and vancomycin also
Adverse effects of trimethoprim/pyrimethamine
Oral trimethoprim can cause bone marrow suppression, resulting in aplastic anemia, leukopenia, and granulocytopenia, pyrmethamine can have similar toxicity
MOA of FQs
Rapidly inhibit bacterial DNA synthesis by inhibiting DNA gyrase and topoisomerase 4
2nd generation FQ
Cirpofloxacin
Ofloxacin
3rd generation FQs
Levofloxacin
4th generation FQs
Gatifloxacin
Moxifloxacin
Besifloxacin
Topical ophthalmic indications of FQs
Contact lens realted ulcers, corneal abrasions, and bacterial conjunctivitis
Systemic indications of FQs
Ciprofloxacin is RXed for gram - urinary and GI infections. Moxifloxacin is approved for the treatment of pneumonia, sinusitis, and intracranial-abdominal and skin infections
Adverse effects of FQs
ORAL fluroquinoLONES can hurt the attachment to your BONEs; causing tendinitis. Oral FQs are contraindicated in pregnancy, chidlren, and adolescents below the age of 18 due to damage in cartilage formation and inhibition of bone growth
Effectiveness of the differnt generations of FQs
There are 4 generations, 3 and 4 have been formulated with improved effectiveness against gram + infections, however these drugs continue to be potent against gram - bac as well
Topical FQs and kids
All of the TOPICAL (NEVER ORAL) FQs are approved for kids 1 year and older EXCEPT LEVOFLOXACIN
Bacteriostatic agents
Tetracyclines, trimethoprim, sulfacetamde, and to some degree, erythromycin
Bacteriocidal agents
PNS, Cephs, bacitracin, aminoglycosides, FQs
Number one symptom of TB
Night sweats
TB is caused by
Mycobacterium TB
Active TB
Treated with a combo therapy
Latent TB
Treated with isoniazid or rifampin monotherapy
Active TB treatment is
RIPE
- rifampin
- isoniazid
- ethambutol
Don’t need to know the P one
TB=RIPE Cheese
RIPE for the drugs
Cheese=caseous necrosis
MOA of rifampin
Prevents mRNA synthesis (transcription) by binding to the beta subunit of DNA dependent RNA POLYMERASE
Adverse effects of rifampin
Hepatotxicity (increased AST and ALT), orange/pink colored tears and urine
Isoniazid MOA
Prevents cell wall synthesis by inhibiting mycolic acid synthesis
Adverse effects of isoniazid
Hepatotoxicity, can also cause pyridoxine (vit B6) deficiency that may result in peripheral neuropathy. Rarely It can cause optic neuritis and optic atrophy, resulting in loss of vision
Ethambutol MOA
Inhibits synthesis of mycobacterium cell wall by inhibiting arabinosyl transferase
What are the two drugs that can be used in isolation for TB monotherapy (latent)
Rifampin
Isoniazid
Adverse effects of ethambutol
Optic neuritis (retrobulbar) May be reversible vision loss
What TB drug is known to cause retrobulbar optic neuritis
Ethambutol
Antivirals for the flu
Oseltamivir (tamiflu)
-inhibits influenza A and B viral neuraminidase
Conjunctivitis due to influenza in 1% pts has been reported
MOA of HIV therapy (Zidovudine [Retrovir])
Reverse transcriptase inhibitor
AIDs occurs at what CD 4 count
<200
Clinical indications of zidovudine (Retrovir)
Major component of three-drug therapy for HIV. Also used during pregnancy to lower the risk of transmitting HIV to the fetus (vertical transmission)
Adverse effects of zidovudine (Retrovir)
- Bone marrow suppression
- Lactic acidosis
- Muscle breakdown
Amblyopia and macular edema have also been reported
There is a vax for which Heps
A and B
None for C
Hepatitis C therapy
C=chronic
Ribavirin + interferon
MOA of ribivirin
Inhibits viral RNA polymerase
Always in combo with interferon for the treatment of hep C
Adverse effects of ribavirin
Conjunctivis
Retinopathy
Retinal vascular Occlusions
Ocular side effects of ribavirin
RIBAViriN RD Ischemia Bleeding Arterial and Venous occlusions Optic Neuritis
VA normally OK
Why kind of virus is herpes
DNA
What do all herpes meds do
Inhibit DNA polymerase
Trifluridine MOA
Inhibits DNA polymerase for the treatment of herpes simplex keratitis
Not used often because 9x day dosing and thimerosol
Acyclovir, valacyclovir, famcyclovir MOA
DNA polymerase inhibitors
Indications of acyclovir, valacyclovir, and famcyclovir
Cold sores, genital sores, and shingles. They may also be RXed for HZO, HSV keratitis, and prophylaxis against recurrent HSV keratitis
Adverse effects of acyclovir, valacyclovir, and famcyclovir
Headaches and GI effects
Renal dysfunction
-be careful in those with renal dysfunction and the elderly. Monitor closely
Oral antivirals
Used to treat HSV epithelial keratitis, but topical ophthalmic treatment is considered the standard of care. Oral dosages should be decreased in patients with kidney disease
Gancylovir
- DNA polymerase inhibitor
- reduced corneal toxicity, 5x/day dosing (better than viroptic)
- BAK instead of thimerosol
Clinical indications for gancyclovir
HSV keratitis
Intraocular sustained-release capsule for the treatment of CMV retinitis
CMV
Opportunistic infection
Vision threatening retinopathy in those with AIDS
-most common intraocualr infection in patients with AIDs
-treat with Zirgan (gancyclovir), if that doesnt work, use your safety “net” Foscarnet
Foscarnet
- SAfety net for CMV if gancyclovir fails
- DNA polymerase inhibitor, IV
- nehprotoxicity and seizures
Fungal ucler
Feathery edges
Immunocompromised
Chronic beat up cornea
Tree branch
Fungus: ergosterol
Component of fungal cell membranes that is not found in human or animal cell walls.
Antifungal drugs
Natamycin, amphotericin B, nystatin
Ketoconazole, fluconazole, and miconozole
Griseofulvin
MOA of natamycin, amphotericin B, and nystatin
Bind to ergosterol and form pores
Clinical indictions for natamycin
Approved for the treatment of fungal blepharitis, conjunctivits, and keratitis caused by susceptible organisms of Candida, Aspergillus, and Fusarium
Clinical indications for Amphotericin B
Broad spectrum antifungal.
Fungal keratitis, and IV form to treat systemic and intraocular fungal infections.
Nephrotoxicity is common in IV form
Clinical indications of Nystatin
Candida oral (thrush) and vaginal (yeast) infections Not indicated for ophthalmic use
MOA of ketoconazole, fluconazole, and miconazole
Inhibit ergosterol synthesis
Clinical indications of ketoconazole
First oral azole antifungal drug and is indicated for the treatment of severe fungal corneal ulcers, systemic fungal infections, and acanthoemeba
Indications of fluconazole
Orally, topically, or through subconjunctival injections
Adverse effects of the azoles
Hepatotoxicity
MOA of griseofulvin
Inhibits fungal mitosis by interfering with microtubule formation
Clinical indictions of griseofulvin
Scalp and skin, fingernails and toenails
Treatment of toxoplasmosis
Sulfadi + pyrimethamine
Antiparasitic drugs
Chloroquine
Lindane
MOA of chloroquine
- Results in the build up of heme within the RBCs; this accumulation is toxic to the “intra-erythrocytic” plasmodium parasite responsible for malaria
- Inhibits phosphlipase A2 to decrease inflammation, not generally used for this
Adverse effects of chloroquine
Whorl K
Bulls eye maculopathy: granular hyperpigmentation surrounded by zone of depigmentation
Binds melanin=migration of RPE cells-permanent
What does a plaquenil screening consist of
10-2 VF
SD-OCT
Why does chloroquine cause bulls eye maculopathy
Binds to melanin of the RPE cells, causing localized RPE damage and subsequent migration of RPE cells to the outer nuclear and OPL. The initial sign of bulls eye maculopathy is RPE mottling within the macula
Risk of developing bulls eye maculopathy in chloroquine
- > 2.3mg/kg body weight (Hydroxychloroquine is >5mg/kg)
- treatment > 5 years
- abnormal renal function
- high body fat
- > 60yo
- liver disease
- concomitant retinal disease
Scotomas of chloroquine
Central and paracentral most common
Lindane
Antiparacytic MOA: lipophlic structure absorbed through the exoskeleton of insects, resulting in seizures and death -lice, scabies -causes conjunctivits -not for the eyes
What is the first step in the arachidonic pathway
Phospholipase A2
What are leukotrienes synthesized by
Lipoxygenase
Thromboxanes
Induce platelet aggregation
COX2
Synthesizes PGs that mediate inflammation
- pain
- fever
- swelling
COX1
Synthesizes PGs that inhibit gastric secretions and influence gastric motility
-protects our ONE stomach
MOA of hydroxychloroquine (plaquenil)
- Inhibits phospholipase A2
2. Build up of heme
Clinical indications for hydroxychloroquine
Lupus
RA
Malaria
Adverse effects of hydroxychloroquine
Corneal deposition (whorl K) Bulls eye maculopathy (greatest threat to vision)
Ideal daily dose of hydroxychloroquine
toxic I’d >5mg/kg body weight
Do not exceed 400mg per day
Toxic dose of chloroquine
> 2.3mg/kg body weight
Risk factors for maculopathy in hydroxychloroquine include
Treatment duration > 5 years Abnornal renal function Liver disease Age > 60 High body fat Concomitant retinal Disease
Baseline exam for hydroxychloroquine
- baseline dilated retinal exam within 1 year of beginning drug.
- annual screenings initiated after 5 years
- 10-2 HVF, SD-OCT
- if patient is at a greater risk of development of bulls eye maculopathy, exams should occur every 6 months to 1 year after the baseline exam.
- risk much higher with chloroquine than hydroxychloroquine
- 2.3mg/kg chloroquine and 5mg/kg hydroxychloroquine
Which is more toxic, chloroquine or hydroxychloroquine
Chloroquine
Strong topical steroids
Pred acetate
Rimexolone
Difluprednate
Dexamethasone
Weak topical steroids
Loteprednol
Fluorometholone (FML)
What are the systemic steroids
Fluticasone
Triamcinolone
Hydrocortisone
MOA of steroids
Inhibition of phospholipase A 2
Steroids side effects
Increased blood sugar Insulin resistance Peptic ulcer (decreased PGs) Decreased fibroblasts (decreased healing) Osteoporosis HTN Psychiatric
Ocular side effects of steroids
PSC cataracts (dose dependent, irreversible)
Glaucoma
Increased risk of secondary infections (HSV K)
Central serous chorioretinopathy
What to inquire about before RXing oral steroids
Pregnancy
Peptic ulcers
Diabetes
Hydrocortisone RXed for
Adrenal insufficiency
May also be used as a potent anti inflammatory medication
What steroid should not be give to dark skinned patients
Triamcinolone
Ophthalmic indications of triamcinolone via injection
- DM mac edema
- graves
- intermediate or non resolving posterior uveitis
- chalazia
- recalcitrant Irvine gass CME
- CME associated with noninfectious posteiror uveitis
- mac edema secondary to CRVO
Systemic indications for triamcinolone
Dermatoses
Asthma
exacerbations of MS
Arthritis
Adverse effects of triamcinolone
Elevated IOP (decreased TM outflow) Endophthalmitis Depigmentation of the eyelid skin in darker skinned patients (permanent)
Fluticasone
Steroid Intrnasal corticosteroid (topical) indicated for treatment of allergic rhinitis
Adverse effects of fluticasone
Cataract, increased IOP, conjunctivitis, and dry eye disease, CSCR
Topical NSAIDs
Diclofenac Nepfenac Bromfenac Ketorolac Flurbiprofen
Oral NSAIDs
Aspirin
Indomethacin/ibuprofen/naproxen/naproxen sodium/piroxicam
Celecoxib
What is the only irreversible COX 1 and 2 inhibitor
Aspirin
MOA of apirin
Salicylate that inhibits the synthesis of PGs and thromboxanes by acting as an irreversible COX 1 and 2 inhibitor
Clinical indications of Aspirin
Antipyresis (fever)
Anti-inflammtory effects
Analgesia
Reduces the risk of recurrent heart attacks in pts with heart disease
Adverse effects of aspirin
GI effects (decreased COX1=increased acid) Antiplatelet effects=bleeding complications in the eye (retinal and subconjunctival heme) Reye’s syndrome in kids
What are the reversible COX 1 and 2 inhibitors
Indomethacin Ibuprofen Naproxen Sodium naproxen Piroxicam
Clinical indications for Indomethacin Ibuprofen Naproxen Sodium naproxen Piroxicam
Scleritis and episcleritis
Indomethacin Ibuprofen Naproxen Sodium naproxen Piroxicam Contraindicated in
Patients with heart disease
Adverse effects of Indomethacin Ibuprofen Naproxen Sodium naproxen Piroxicam
All increase the risk of bleeding complications in the eye
Risk if GI bleed
Fatal MI/stroke
Which NSAIDs are safe for pateitns with cardiovascular disease
Aspirin ONLY
Indomethacin Ibuprofen Naproxen Sodium naproxen Piroxicam ALL contraindicated in heart disease patients. Can increased BP
Which NSAIDs can cause Reye’s syndrome
Aspirin ONLY
Indomethacin Ibuprofen Naproxen Sodium naproxen Piroxicam DO NOT
Which NSAID can be safely RXed in kids 6m and older
Ibuprofen
What should NSAIDs be taken with in order to decrease effects on GI
Food
Pigmentary retinopathy drugs
Chlorpazamine
Thioridazine
Indomethacin
Ocular side effects of indomethacin
Increases the risk of bleeding in the eye
Whorl K
Retinary pigmentary changes (mottling)
Misoprostol
Synthetic PG E1 that is chemically similar to PGE-2, the PG that protests the stomach lining. It is used for prevention and treatment of NSAID induced stomach ulcers. It’s main adverse effect is that is can cause miscarriages and premature labor
MOA of celecoxib
Selective COX2 inhibitor
Spares the COX1 pathway and protects the stomach
Adverse effects of celecoxib
SJS
Contraindications of systemic NSAIDs
Patients with a history of an allergic reaction to other NSAIDs or to aspirin
Parasympathetic acts on ___receptros
Cholinergic (muscarinic) receptors that target organs; promotes bronchoconstriction, miosis, rest and digest, and increase in secretions (SLUD: salivation, lacrimation, urination, defacation)
Sympathetic acts on _____ receptors
Adrenergic (a and b) receptors on target organs; promotes bronchidilation, mydriasis, a decrease in secretions and fight or flight
Direct cholinergic agonist (ocular)
Pilo
Indirect cholinergic agonists (ocular)
Edrophonium
Echothiophate
Pyridostigmine
Neostigmine
ACHase blockers
Donepizil
CNS ACHase inhibitor that is indicated for the treatment of Alzheimer’s (indirect cholinergic agonsit)
Cholinergic antagonists
- First generation H1 blockers: diphenhydramine, brompheniramine, chlorpheniramine, promethazine
- antipsychotics: chlorpromazine, thioridazine
- antidepressants: TCAs (amitriptyline, imipramine), MAOI (phenylzine)
- muscle relaxant: cylcobenzaprine
- anti-anxiety: diazepam
- ipratropium
Systemic A2 agonist
Clonidine
Systemic B1/B2 agonist
Isoproteronol
Systemic B2 agonist
Salmeterol Albuterol Levabuterol Terbutaline Metaproterenol
systemic B agonists and IOP
Increase aqueous humor production. Salmeterol is the only long acting B2 agonists and the only drug that does not carry a specific warning regarding use in patietns with glaucoma
What is the only long acting B2 agonist that does not have a specific warning regarding use in glaucoma patients
Salmeterol
Nonspecific alpha and beta agonist
Pseudoephedrine
Dopamine agonsits
Bromocripitine
Methylphenidate
Dextroamphetamine
Increase adrenergic acitivtiy, do not give to narrow angle patients
Parkinson’s drugs
Amantadine
Dopamine agonist
Adrenergic agonist, do not give to narrow angle patients
Alpha 1 blockers
Prazosin
Tamsulosin
Terazosin
BPH drugs
B-blockers
Propanolol
Labetolol
Atenolol
Metoprolol
Nonselective B agonsits
Labetolol
Propranolol
B1 specific antagonists
Atenolol, metoprolol
Which BBlockers would have least affect on IOP
BEAM
- betaxolol
- atenolol
- metoprolol
B1 selective
Cold medication is targeted at
Ameliorating symptoms
Pseudoephedrine
Cold medicine
MOA: nonspecific alpha and b agonist for nasal decongestion
Adverse effects of pseudoephedrine
Tachycardia (b1), bronchodilator (b2), nervousness
Ocular: diplopia, and blurred vision, caution with increased IOP (B2)
H1 receptors
In the smooth muscle of the bronchi, blood vessels, and intestines. Activating of H1 causes itching, vasodilation, increased vascular permeability, and contraction of smooth muscel in the GI tract
H2 receptors
Located in the gastric parietal cells, the heart, pulmonary blood vessels, and cells of the immune system. Activation of H2 receptors causes itching, vasodilation, mucous discharge, and gastric secretions
Which H receptor is found in the eye
Mostly H1
Histamine release in the eye
H1 receptors
Itching, tearing, chemosis, dilation of conjunctival blood vessels and papillary reaction.
First generation antihistamines
Diphenhydramine
Chlorpheniramine
Brompheniramine
Promethazine
Which generation of anti histamine drugs causes anticholinergic type reactions in the eye and what are the reactions
First generation
Increased IOP, dry eye, mydriasis
MOA of first generation H1 blockers
Block the interaction between histamine and H1 receptors
Clinical indications of first generation H1 blockers
Allergic skin reactions
Adverse reactions of first generstion H1 blockers
Sedation due to CNS penetration (BBB). All antihistamines especially first generation drugs, have anticholinergic effects including mydriasis, increased IOP, dry eye, dry mouth, and tachycardia
What’s special about promethazine
First generation H1 blocker
Chemical structure similar to antipsychotic medications (phenothiazines)
Ocular side effects specific to this drug result from the phenothiazine structure and include corneal epithelial Keratopathy, corneal endothelial pigmentation, lenticular changes, and pigmentary retinopathy
Second generation H1 blockers
Loratadine
Fexofenadine
Cetirizine
Clinical indications of second generation H1 blockers
Allergic rhinitis, and chronic urticaria (hives)
Adverse effects of secondary generation H1 blockers
Less CNS penetration and less CNS side effects. Cetirizine can cause abnormal EOM contractions (oculogyric crisis)
Majority of peptic ulcer disease is caused by
Helicobacter pylori and/or NSAID use
H2 blockers
Cimetidine
Ranitidine
Famotidine
MOA of H2 blockers
Prevent histamine stimulation of gastric acid (HCl)secretion by blocking H2 receptors on gastric parietal cells
Clinical indications of H2 blockers
Healing and preventing stomach ulcers and acid reflux
Adverse effects of H2 blockers
Diarrhea; cimetidine has numerous drug interactions and can cause gynecomastia and loss of libido
Proton pump inhibitors
Omeprazole
Esomeprazole
MOA of PPIs
Inhibit H+/K+ ATPase (proton) pumps
Clinical indications of PPIs
1st line therapy for peptic ulcer disease and GERD
Sucralfate
Gastric lining protector
MOA: forms a paste like substance by binding to positively charged proteins and damaged ulcer tissue in the stomach.
Adverse effects of sucralfate
Interfere with absorption of other oral medications, dont use within 2 hours of otherdrugs
Bronchodilators stimulate ____ nervous system
Sympathetic
Long acting B2 agonists
Salmeterol
uses of salmeterol
Only long lasting B2 agonist we need to know
Maintenance therapy for COPD and asthma but NOT as a rescue inhaler
Short acting B2 agonsits
Albuterol, levalbuterol, terbutaline
Metaproterenol
Isoproterenol
Clinical indications of albuterol, levalbuterol, and terbutaline
Short acting B2 agonsits
Rescue inhaler for patients with asthma and COPD
Clinical indications of metaproterenol
no longer recommended for asthma due to excessive cardiovascular effects from B1 stimulation
Clinical indications of isoproterenol
No longer RXed for the treatment of asthma. Nonspecific B agonsits primarily indicated for the treatment of arrhythmias through B1 stimulation
Adverse effects of short acting B2 agonsits
They have greater B2 than B1 activity, but the effects come from B1 activity on the heart
-tachycardia, heart palpitations, nervousness, tremors, nausea
Short acting B2 agonsits and IOP
All have warnings about their use in glaucoma patients due to the risk of IOP increase
Muscarinic antagonist for asthma
Ipratropium
- blocks muscarinic receptors
- inhibits bronchoconstricion
- caution in narrow angle glaucoma due to pupil dilation
Miscellaneous respiratory agents
Montelukast and Zafirlukast
Theophylline
Acetylcysteine
Montelukast and Zafirlukast
Leukotriene receptor antagonists
Treat asthma and bronchoconstriction
Montelukast also used for allergic rhinitis
Theophylline
Inhibits PDEs, leading to increase cAMP and increased release of epi.
Narrow TI
BBlockers, including topical ophthalmic agents such as timolol, have the potential to mitigate the bronchodilatory effects of theophylline
Acetylcysteine
Mucolytic agent that breaks disulfide bonds in proteins of mucus in order to reduce its viscosity. The topical opthalmic form can be RXed as QID for filamentary keratitis, dry eye syndrome, and corneal burns
Immunosuppressant medications
Methotrexate
Cyclosporine
Azathioprine
Methotrexate MOA
Inhibits dihydrofolate reductase (like TMP and pyromethamine)which inhibits DNA synthesis
MOA in RA involves immunosuppressant and anti inflammatory mechanisms
Adverse effects of methotrexate
Hepatotoxicty and myelosuppreison, increases the risk of opportunistic infections and lymphomas
Aplastic anemia
Optic neuritis
Cyclosporine MOA
Prevents rejection of organ transplants by inhibiting the release of and production of interluelin-2 (IL-2), a chemical mediator responsible for T lymphocyte activation
Restasis
RXed BID
Inhibits T cell activation by inhibiting production if IL-2
Adverse effects of cyclosporine
Opportunistic infection
Most common cause of reversible posteiror leukoencephalopathy syndrome (RPLS)
Oral cyclosporine
-HA, altered consciousness, seizures, and visual disturbances. DX based on MRI findings. Discontinue if this is diagnosed
Azathioprine
Purine analong that inserts into DNA and RNA and stops replication
Used for RA and to prevent rejection of kidney transplant, ocular MG
Tamoxifen
- a competitive partial agonsit inhibitor of estradiol, which inhibits estrogen effects at the breast
- treatment for breast cancer
Adverse effects of tamoxifen
-crystalline retinopathy, whorl Keratopathy, thromboembolism (BRVO, CRVO)
Cessation of tamoxifen and whorl K and crystalline maculopathy
Whorl K is generally reversible but maculoapthy can affect vision and is not always reversible
Analgesics
OTC agents such as NSAIDS and acetaminophen. RX includes some NSAIDs, muscle relaxants, and tramadol
Non opiate analgesics
Acetaminophen
Cyclobenzaprine
Tramadol
MOA of acetaminophen
Not completely understood
DOES NOT HAVE ANTI INFLAMMATORY PROPERTIES
What is the max amount of acetaminophen you can take in a day
4000mg
Who can take acetaminophen
Anyone
Kids and pregs too
Adverse effect of acetaminophen
Hepatotoxicity
TylenoL=liver metabolism
Cyclobenzaprine MOA
Muscle relaxant
Inhibit alpha and gamma motor neurons
Clinical indications for cyclobenzaprine
Muscle spasms
Adverse effects of cyclobenzaprine
Drowsiness, loss of coordination, and anticholinergic effects; caution in pateitns with narrow angle glaucoma
Dry eye, mydriasis, increased IOP
MOA of tramadol
Acts on Mu opiate receptors (although not considered a true opiate)
Inhibits serotonin and NE uptake within ascending pain pathways
Adverse effects of tramadol
Dry mouth
Sedation
Dizziness
Nausea
Opiate analgesics
Meperidine, oxycodone
MOA of meperidine/oxycodone
Agonists of the Mu, Kappa, and Delta opiate receptors
Adverse effects of opiate analgesics
Pin point miosis
Mydriasis with withdrawal
Naloxone
Opioid antagonsit that is used to reverse the effects of opiates
Migraine therapy
Sumatriptan
MOA of sumatriptan
5-HT1B and 1D (serotonin subtype 1B and 1D) receptor agonists.
Vasoconstriction of cranial arteries
Reduces inflammation in the CNS
Adverse effects of sumatriptan
NAION
Retinal artery occlusions and retinal venous thrombosis
ANTIpsychotics
PHenothiazines
- chlorpromazine
- thioridazine
MOA of antipsychotics (chlorpromazine, thioridazine)
Dopamine receptor antagonists
Adverse effects of antipsychotics (chlorpromazine, thioridazine)
High doses can result in Parkinson’s like effects. Ocular side effects include
- pigmentation effects: pigment on the corneal endothelium, anterior stellate catracts, and hyperpigmentation of the RPE (promethazine also, 1st gen H1 blocker)
- anticholinergic effects: dry eye, mydriasis, and increased IOP
- oculogyric crisis (also Zyrtec)
Parkinson’s disease
Dopamine deficiency TRAP -tremor at rest -rigidity -akinesia (hard time initiating movement) -postural reflexes lost
Antiparkinsons drugs
Amantadine
Bromocriptine
Amantadine
Parkinson’s
-potentials dopamine effects by blocking its reuptake or augmenting it’s release in the brain
Bromocriptine
Parkinson’s
-a dopamine agonsit that is most commonly used to treat prolactin secreting pituitary adenomas. But can also be used to treat parkinsons
Bromocriptine can treat what conditions
Parkinson’s
Pituitary adenoma
ADHD meds
Methylphenidate, dextroamphetamine
MOA of methylphenidate and dextroamphetamine
Increase dopamine release
Clinical indications for methylphenidate and dextroamphetamine
ADHD, narcolepsy, and depression
Adverse effects of methylphenidate and dextroamphetamine
Mydriasis and dry eyes
Caution in acute angle glaucoma
All medications that act as dopamine agonists in the CNS (ADHD and parkinsons drugs) and narrow angle glaucoma
Have adrenergic agonist side effects any may cause mydriasis that can precipitate angle closure in patients with narrow angles. For this reason, narrow angle glaucoma is a contraindication for these medications
Donepizil
- CNS ACHase inhibitor (like MG) that is RXed for alzheimers
- will cause lower IOP due to muscarinic effects. Sudden discontinuation of the drug may lead to elevations in IOP
What are the 4 main classes of antidepressants and what do they all ultimately do
TCAs
MAOIs
SNRI
SSRI
Increase serotonin
TCA, SNRI, and MAOIs also increase NE
What are the side effects of all antidepressant drugs
Sedation, weight gain, and sexual dysfunction
The primary method of treating depression involves
Increased serotonin levels in the CNS. Serotonin selective reuptake inhibitor are the first line treatment for depression
What is the first lien treatment for depression
SSRIs
Which antidepressants increase dopamine
NONE
what are the SSRIs
Fluoxetine
Escitalopram
MOA of SSRIs
Fluoxetine and escitalopram
-inhibits serotonin reuptake
Adverse effects of SSRIs
Fluoxetine and escitalopram
- fewer side effects compared to other anti depressants. They can cause mydriasis and should be used with caution in narrow angle glaucoma patients
- serotonin syndrome may occur if Rxed with TCAs and especially MAOIs
Serotonin syndrome
Due to excess serotonin activity in the CNS and is marked by a change in mental status (anxiety, confusion), autonomic hyperactivity (increased BP, pulse, temp), and neuromuscular problems (tremor, hyperreflexia)
What are the SNRIs
Venlafaxine
Duloxetine
MOA of SNRIs
Venlafaxine and duloxetine
Inhibits serotonin and NE reuptake
Bupropion
Is an NDRI (inhibits the reuptake of dopamine and NE) and is RXed to treat depression and smoking cessation
What are the TCAs
Amitriptyline
Imipramine
MOA of TCAs
Amitriptyline and imipramine
Inhibitions NE and serotonin reuptake
Adverse affected of TCAs
Amitriptyline and imipramine
Dry eye, increased IOP, blurred vision, and mydriasis. A TCA overdose is LIFE threatening. DO NOT RX FOR SUICIDAL PATIENTS
What antidepressant should you never RX for a suicidal patient
TCAs, fatal overdose
What is the MAOI
Phenelzine
MOA of MAOI
Phenelzine
Inhibits MAO, the enzyme responsible for breaking down NE and serotonin
Adverse effects of MAOI
Phenelzine
Glaucoma and nystagmus are reported ocular affects, caution in narrow angles
Foods with tyramine (wine, cheese, dried meats) cause lethal hypertensive crisis
What drugs can exacerbate systemic effects of topical ophthalmic phenylephrine and other adrenergic agonists
MAOIs and TCAs
ANTIanxiety medication
Diazepam
MOA of diazepam
ANTIanxiety
Opens chloride channels by binding to GABA receptors
GABA and anxiety
Increased GABA=decreased sympathetic activity
**increased sympathetic paradoxical effect in extreme populations
Adverse effects of diazepam
Antianxiety drug
- sedation, depression, confusion, bradycardia, and dyspnea; can be fatal if combined with alcohol or drugs. Occasionally cause mydriasis and nystagmus. Caution in narrow angle glaucoma
- increased sympathetic paradoxical effect in extreme populations
What are the anticonvulsants
Phenytoin
Phenobarbital
Topiramate
Phenytoin MOA
Anticonvulsant
-acts on multiple NTs including NE, ACH, and GABA
Adverse effects of phenytoin
Nystagmus, diplopia, EOM palsies, ataxia, and gingival hypoplasia
Funny-toin=funny looking eyes and gums
Phenobarbital
Anticonvulsant
- reduces glutamatergic excitatory transmission by blocking AMPA receptors
- mydriasis, increased IOP, and cycloplegia
Topiramate
Anticonvulsant
-MOA: multiple CNS effects that prevent seizures
Adverse effects of topiramate
Blurred vision, diplopia, nystagmus, myopic shift (huge shift, not permanent)
May cause choroidal swelling, which moves the uvea forward and results in acute secondary angle closure glaucoma
MOA of insulin
Binds to cell surface receptors, leading to activation of tyrosine kinase receptors and a phosphorylation cascade; it promotes the formation and storage of glycogen, proteins, and triglycerides within the liver, fat, and muscle tissue. The primary signal for insulin release is the presence of glucose in the blood
Oral agents for diabetes
Biguanides: metformin
Sulfonylureas: glipizide, glyburide, chlorpropamide
Thiazolidinediones: pioglitazone, rosiglitazone
MOA of Biguanides
Metformin
-decreases gluconeogensis in the liver and increases glucose uptake; it is usually the first oral medication RXed for DM because it DOES NOT CAUSE HYPOGLYCEMIA
Which diabetes medication does not cause hypoglycemia
Metformin
Adverse effects of metformin
Diarrhea, if patient has renal insufficiency or hepatic impairment they are greater risk of lactic acidosis
MOA of sulfonylureas
Glipizide, glyburide, chlorpropamide
-increase the secretion of insulin by beta cells in the pancreases, decrease glucagon release, and increase the sensitivity of cells to insulin
Adverse effects of sulfonyureas
Glipizide, glyburide, chlorpropamide
- hypoglycemia
- caution in those with sulfa allergies
Beta blockers and DM
Increase the risk of hypoglycemia if taken with sulfonyureas. They may also mask the sympathetic response to hypoglycemia caused by any diabetic medication, as they prevent the usually symptoms associated with hypoglycemia such as tachycardia and tremors. The risk is lower, but still exists, with ocular beta blockers
MOA of thiazolidinediones
Pioglitazone, rosiglitazone
- Active peroxisome proliferator-activated receptor gamma
- combat insulin resistance
Adverse effects of thiazolidinediones
Pioglitazone and rosiglitazone
-new or worsening macular edema
What does TSH do
Released from the anterior pituitary gland and binds to TSH receptors on the thyroid glandin the neck, stimulating the production of thyroid hormones (primarily T4). Hashimotots is an AI condition that is the most common cause of primary hypothyroidism, and requires a replacement of T4
Levothyroxine
Synthetic T4 hormone
Can cause pseudotumor cerebri in kids
Used for hypothyroidism (hashimotos)
Adverse ocular effects of estrogens
Dry eyes ON disease (optic neuritis, pseudotumor cerebri, papilledema) Venous clotting (CRVO/BRVO)
What is the class of drugs used to treat erectile dysfunction
PDE-5 inhibitors
What are the PDE-5 inhibitors
Sildenafil and vardenafil
MOA of PDE-5 inhibitors
Sildenafil and Vardenafil
-cGMP, which is broken down by PDE-5, relaxes vascular smooth muscle in the penis during an erection. These drugs inhibit PDE_5, thereby increased blood flow to the penis by prolonging the effects of cGMP=vasodilation
Systemivside effects of PDE-6 inhibitors
Flushing and HA are common; priapism may occur and requires immediate medical attention
Ocular adverse affects of PDE-5 inhibitors
Cyanopsia, blurred vision, and photosensitivity
-due to minor PDE-6 inhibition, which is found in rods and cones
Link between ED meds and NAION
There is an increased incidence of NAION in men taking ED meds, but they already have reduced blood flow anyways, so not sure if its from the drug or their underlying problem
BPH drugs
Alpha-1 blockers
-prazosin, terazosin, tamsulosin
MOA of BPH drugs (zosins)
A1 blocker to relax smooth muscle in the bladder neck and prostate, thereby decreasing urinary outflow obstruction in men with BPH
Adverse effects of BPH meds (zosins)
Interoperative floppy eyelid syndrome from tamsulosin (flomax)
What are the classes of antihypertensive medications
ACE inhibitors Angiotensin II receptor agonists (ARBS) BBlockers Ca Channel blockers Diuretics Clonidine Hydralazine
ACE inhibitor drugs
Lisinopril
Benazepril
Enalapril
Captopril
MOA of ACE inhibitors
- Prevent the formation of angiotensin II by inhibiting angiotensin converting enzyme (ACE)
- Block the metabolism of bradykinins, resulting in vasodilation
Adverse effects of ACE inhibitors
Cough
Angiotensin II receptor agonist (ARBs)
Losartan
MOA of losartan
Reduces BP by inhibiting angiotensin II directed contraction of vascular smooth muscle and stimulation of aldosterone secretion
What’s better about ARBs than ACE inhibitors
No cough
What are the BBlockers used for HTN
Propranolol, labetalol
metoprolol, atenolol
Propranolol and labetalol MOA
Non selective beta 1 and beta 2 receptor antagonists; they also block the release of renin from the kidneys
MOA of metoprolol and atenolol
Selective B1 receptors agonists
Less IOP effect here
“MA on the heart”
CNS effects of BBlockers
Disorientation, depression, fatigue
Cardiovascular effects of BBlockers
Bradycardia, arrhythmias, syncope
Pulmonary affects of BBlockers
Dyspnea, wheezing, bronchospams
GI effects of BBlockers
Nausea, vomiting, diarrhea, abdominal pain
Reproductive effects of BBclokers
ED
What are the calcium channel blockers
Nifedipine
Verapamil
Diltiazem
MOA of Ca channel blockers for HTN
Verapamil, diltiazem, nifedipine
-block L type Ca channels, resulting in a marked decrease in intracellular free Ca2+
Ca and smooth muscle
Decreased Ca and decreased smooth muscle contraction
Cardio affects and Ca channel blockers
Verapamil and diltiazem more commonly have direct cardio effects
“VD-dipines”
Heart——>BV
Ca Channel blockers and glaucoma
Some studies have suggested prescribing Ca channel blockers for the treatment of low tension glaucoma, as these drugs may increase perfusion to the optic nerve, how ever, this is not considered standard of care
What part of the nephron do CAIs work
PCT
What part of the nephron do HCTZ/CTZ work
DCT
What part of the nephron does furosemide work in
Ascending loop of henle
What part of the nephron does triamterene and spironolactone work
Collecting duct
What is reabsorbed in the PCT
Bicarbonate, Na, H20
What is reabsorbed in the descending loop of Henle
Last place H20 is reabsorbed without hormone help
What reabsorbed in the DCT
Na, chloride
What is reabsorbed in the ascending loop of henle
Na, Cl, K
What is reabsorbed in the collecting duct
H20 with the help of aldosterone
What part of the nephron does mannitol work
Works across the entire nephron
What diuretic can cause hypokalemia
Furosemide
Diuretics can treat
CHF, HTN, kidney disease
What is the loop diuretic
Furosemide
MOA of furosemide
Inhibits Na/2Cl-/K+ co-transporter in the thick ascending loop of henle. It also increased CA2+ secretion
Adverse effects of furosemide
Hypokalmiea
Nephrotixicity
Ototoxicity
MOA of the thiazides (HCTZ/CZ)
Inhibits NaCl reabsorption and decreased CA2+ excretion at the early DCT
Adverse effects of thiazides
Acute transient myopia and acute angle closure glaucoma
What are the potassium sparing diuretics
Spironolactone and triamterene
Aldosterone stimulation
Aldosterone release is stimulated in response to decreased blood volume (angiotensin II) and increased K+ concentration. It increases Na+ reabsorption and K+ secretion in the collecting duct by opening epithelial sodium channels (ENaCs) and by activating the Na+/K+ ATPase pumps. The net effect is increased Na+ and Cl- reabsorption, and increased K+ and H+ secretion
What the weak diuretics
Sprinolactone
Triameteren
MOA of spironolactone
Blocks the action of aldosterone at the late DCT and collecting duct
Adverse effects of spinrolactone
Hyperkalemia, gynecomastia, and antiandrogen effects
MOA of triamterene
Directly blocks ENaCs in the late DCT and the late collecting ducts
Does not have antiandrogen effects like spironolactone
Mannitol
Osmotic diuretics
-incapable of being absorbed
What diuretics can cause dry eye
All of them
Clonidine MOA
CNS a2 agonist that decreases sympathetic outflow and increases parasympathetic tone, resulting in decreased vascular resistance and decreased heart rate
Adverse reaction of clonidine
Dry mouth, sedation, impotence, and severe rebound HTN
What other drug is clonidine related to
Apraclonidine
It could decreased IOP
MOA of hydralazine
Increases cGMP, resulting in smooth muscle relaxation; it also decreases afterload as it vasodilates arterioles more than veins
Adverse effects of hydralazine
Compensatory tachycardia, fluid retention, and lupus like syndrome, conjunctivitis and increased lacrimation have also been reported
Digoxin MOA
Inhibits the Na+/K+/ ATPase enzyme, which normally pumps Na+ out and K+ in; this leads to increased intracellular Ca2+
Adverse effects of digoxin
Retrobulbar optic neuritis, BY color defects, and entropic phenomenon (snowy vision), blocks NAK channels in the PR
Drugs to treat CHF
Digoxin
BBlockers
ACE inhibitors
Diuretics
Amiodarone
Antiarrythmic drug
-primarily blocks K+ channels, but also blocks some Na+ and Ca2+ channels as well
Clinical indications of amiodarone
Arrhythmias
Adverse effects of amiodarone
- NAION
- Whorl K
- Anteiror supcasular lens deposits
Anticoagulants
Warfarin
Clipidogrel
Dipyridamole
Warfarin
Vitamin K antagonist
Interferes with clotting factors 2, 7, 9, 10
What drug is contraindicated in patietns taking anticoagualtans
Cephs
Adverse effects of warfarin
Should be stopped 96-115 hours prior to cataract surgery
Contraindicated in pregnancy and may also result in skin necrosis
How can warfarins effects be reversed
Vit K
Clopidogrel
Inhibits ADP receptor on platelet cell membranes that is needed for platelet aggregation and clot formation
Adverse effects of clopidogrel
Irreversible effect on platelets (like aspirin)
Dipyridamole
Inhibitions adenosine deaminase and PDE, resulting in the accumulation of cGMP and adenosine, which inhibits platelet aggregation and may cause vasodilation
Adverse effect os dupyridamole
Aggrenox=this + aspirin
Risk of bleeding
Meds that can cause bleeding problems in the eye
Warfarin Clopidogrel Dipyridamole NSAIDs Aspirin
Antihyperlipidemic agents
- HMG CoA inhibitors
- Fibric acid
- bile acid binding resin
Lovastatin, simvastatin, atorvastatin
HMG CoA reductase inihibitors
-Rate limiting step in cholesterol synthesis in liver
Lower LDL and trigs, and increase HDL
Fibric acid for HDL
Gemfibrozil
Gemfibrozil MOA
Binds to PPAR-a and increases the activity of lipoprotein lipase, which breaks down VLDL.
Lowers LDL and trigs (does not increase HDL)
Cholestyramine
Bile acid binding resin
- prevents bile acid reabsoprtion for HLD control
- lowers LDL levels (does not increase HDL or lower trigs)
MOA of isotretinoin
Reduces the size and degree of oil production from sebaceous glands
-affects meibomian glands
Adverse effects of isotretinoin
Blepharoconjunctivitis
Dry eyes
pseudotumor cerebri
Also teratogenic and contraindicated in pregnancy
Metronidazole
NOT FOR USE ON EYES
-topical agent RXed for acne rosacea, disrupts DNA and inhibits nuclei acid synthesis; also has anti-inflammtory properties
Alcohol withdrawal
Can be life threatening
Alcohol and vitamin deficiency
Chronic alcoholics can lead to thiamine deficiency (B1), resulting in an acute presentation of Wernickes encephalopathy, which is characterized by ophthalmoplegia, confusion, and ataxia. Untreated thiamine deficiency can lead to irreversible korsakoff syndrome, which is characterized by amnesia and confabulation
Give them B1 and this goes away (except korsakoff)
Opioid withdrawal
Not life threatening
Pin point pupils when they are on it, mydriasis when they are going through withdrawal
Cocaine addiction
Mydriasis
Withdrawal is not life threatening
