What is the most commonly prescribed medication for glaucoma?
Litanoprost
Brimaprost (same class)
What is the primary underlying cause of glaucoma?
increased IOP
When treating glaucoma, what are the 4 classes of drugs that could be effective?
Prostaglandin analog
Beta 2 antagonist
Carbonic anhydrase inhibitor
Parasympathomimetic (muscarinic agonist, cholinesterase inhibitor)
What class is acetylcholine? Which condition can be treated by this?
parasympathomimetic -muscarinic and nicotinic agonist
-Myasthenia Gravis - increases available ACh, can produce sk. m. contraction.
What class is acyclovir?
anti-viral agent
Acyclovir inhibits which aspect of viral replication? What is special about this pharmacologic agent?
guanosine analog; incorporates into the viral DNA and inhibits further synthesis
- can cross BBB, used in herpes meningitis and encephalitis*
- although, gen. used topically for HSV 1 and 2
Albuterol, one of the most important drugs in pharmacology, is in which class? What advantage does it have over other agents in this class?
beta 2 agonist (bronchodilator)
- selective! will not produce effects on myocardium
(most asthma pts cannot tolerate tachycardia s/e)
Amiodarone is in which class and what is it’s MOA?
Class 3 anti arrhythmic
- K channel blocker
What are the two ways in which bacteria can become resistant?
- bacteria can develop beta-lactamase (enzyme against the B-lactam ring in certain antibiotic classes)
- PBP can change conformation and stop specific antibiotics from binding
Penicillins and cephalosporins both contain this specific aspect in their drug class? what does it do?
beta-lactam ring
- inhibits formation and repair of bacterial cell wall
i. e. bactericidal
How can we prevent bacteria from becoming resistant to the effects of a beta-lactam ring? which drug is this represented by?
by adding CLAVULINATE
- prevents formation of beta-lactamase
- Amoxicillin-clavulinate; Augmentin
which drug class is amphotericin B in and what is it’s MOA?
anti-mycotic agent
- MOA – binds to ergosterol in fungal cell membrane forming pores (pokes holes = cell death)
saved for life threatening fungal infections, IV, inexpensive.
What side effect is amphotericin B known for? How do you prevent this?
Shake and Bake
- fever, chills, N/V, renal toxicity
Pre-emptively prescribe aspirin, anti-pyretics, and anti-histamines
How do the -azoles work in regard to fungal infection?
anti-mycotic that prevent formation of ergosterol
fungal-static
Atenolol is in which drug class, what is it’s MOA?
parasympatholytic - selective beta 1 antagonist (cardio-specific)
- negative ionotrophic and chronotrophic effects i.e. reduce timing and force of contraction
What are the two ways to alter hypertensive states?
PR x CO = BP
reduce peripheral resistance (hydration [depending on cause], anti-coagulants/blood thinners)
or
reduce cardiac output (atenolol)
atrovastatin is in which class and what is its class's MOA? What is a common S/E for this drug? How do we try to alter it, although not proven by science?
statin, HMG-CoA reductase inhibitor
S/E - myopathies
supplement with CoQ10
Atropine is in which drug class and what is it’s MOA?
parasympatholytic
MOA - muscarinic antagonist
i.e. - inhibits SLUD*
what muscarinic antagonist is used exclusively to treat respiratory illness such as: asthma and COPD?
Ipratroprium (Atrovent)
Which drug class is azithromycin in and what distinguishes this drug?
MACROLIDE antibiotic
- Z- PACK (5 day, concentration dependent course with front load on the first day)
bacteristatic
What S/E is commonly seen in the macrolides erythromycin and azithromycin? Which of the two examples exhibits lower likelihood of side-effects?
DIARRHEA
Azithromycin has less side-effects
Bethanechol is in which drug class and what is it generally used to treat?
parasympathomimetic, muscarinic agonist
used to treat paralytic bowel or paralyzed urinary bladder (i.e. causes SLUD)
Carvedilol’s class and MOA, go!
Sympathomimetic
non-selective Beta Blocker (beta 1 and 2 antagonist), selective alpha 1 antagonist
What is carvedilol used to treat?
heart failure (mild to severe) and hypertension - could prevent second MI
What class is cephalexin in and what is the MOA? Because of its class and MOA, you know it has a _____.
class: cephalosporin antibiotic
MOA: binds PBP proteins inhibiting bacterial cell wall synthesis
B-lactam ring!
What is cephalexin used to treat?
bacterial infections - URI, UTI, skin, ear, genital
- alternative in patients with penicillin allergy
What is the class and MOA of clopidogrel?
prodrug, metabolized by cyp450 to active form
inhibits platelet activation and aggregation
irreversibly binds P2Y12 class of ADP receptors on platelets.
Clopidogrel is used to treat?
used for MI and stroke prevention
commonly prescribed post MI, stroke, or peripheral vascular disease.
used with aspirin to treat new/worsening chest pain (MI, unstable angina) works to dilate blood vessel
What is the MOA of digoxin? Which class of drugs is it in? And what’s a common S/E?
class: digitalis glycoside; ATPase inhibitor
MOA: inhibits sodium-potassium ATP-ase enzyme regulating quantity of Na+ and K+ inside cells.
S/E - Diuresis
When is digoxin prescribed? When is it C/I? How does it work?
A-fib, CHF (some pts)
C/I if PREVIOUS MI*
It works by increasing the force of contraction (positive ionotrophic effect) and slowing rate (negative chronotrophic).
what is the class and MOA of diltiazem?
class: Ca channel blocker (Class IV anti-arrhythmic); anti-HTN, anti-angina
MOA: prevents Ca from being released; prevents smooth muscle contraction
- heart and periphery
Which antibiotic has the distinguishing characteristic of chelation - i.e. commonly chelates Ca so should not be consumed with dairy products or Ca supplements? Which class of antibiotics also chelates Ca?
Doxycycline
- TOOTH DISCOLORATION C/I CHILDREN
- also causes photosensitivity*
Fluoroquinolones
- broad spectrum
- avoid taking with dairy.
doxycycline, is in which class?
tetracycline antibiotic
MOA: bind 30S ribosomal subunit - bacteriostatic
When is doxycycline indicated?
IND: N. gonorrhea or severe acne
- good alternative to penicillin allergy
what class is epinephrine in? what is the MOA?
class: sympathomimetic
MOA: α- and β-adrenergic receptor agonist
when is epinephrine indicated?
MC tx for anaphylaxis
prolong action of local anesthetics
decreases bleeding
ophthalmic indications
what is the class and MOA of ezetimibe?
MOA: reduces intestinal absorption of cholesterol and sugar
- without affecting absorption of triglycerides or fat-soluble vitamins
when is ezetimibe used?
tx of elevated blood cholesterol
what is the class and MOA of fluconazole?
class: azole anti-mycotic
MOA: decreases ergosterol synthesis; inhibiting cell membrane formation.
when is fluconazole indicated?
fungal (candida, MC) infection
what class is furosemide in and what is it’s MOA?
class: loop diuretic
MOA: acts by inhibiting the Na-K-Cl cotransporter in the loop of Henle (thick ascending limb)
when is the diuretic furosemide indicated for use? what is a s/e we should be aware of?
edema, HTN
S/E - ototoxicity
what class is gentamicin in and what is the MOA?
class: aminoglycoside (broad-spectrum) antibiotic
MOA: inhibit protein synthesis, irreversibly binds 30s ribosomal sub-unit, bactericidal
what are the common s/e we need to be cautious of with gentamicin?
NEPHROTOXICITY OTOTOXICITY (esp w. diuretic rx)** -irreversible HL
what class is hydralazine in and what is the MOA? what is a S/E of this drug?
class: direct arterial vasodilator
MOA: increases cGMP relaxes smooth muscle
S/E - Reflex tachycardia
(lupus like syndrome)
when is hydralazine indicated for use?
severe HTN, CHF
First line therapy for HTN in pregnancy
hydrochlorothiazide - class and MOA
thiazide diuretic
MOA: Inhibits Na and Cl transporters in Ascending and DCT
what is a common s/e of hydrochlorothiazide
hypokalemia, hyponatremia
- also, avoid in patients with sulfa allergy
what class is ipratropium in and what is the MOA?
class: anticholinergic (parasympatholytic)
MOA: Brochodilator
- blocks muscarinic receptor, antagonist of acetylcholine
When is ipratropium indicated?
asthma
What is the number one treatment of glaucoma?
Latanoprost
What is Latanoprost? Class, MOA?
class: prostaglandin analog
MOA: works to decrease IOP by increasing outflow of aqueous humor (prostaglandin F2 receptor agonist)
what is the class and MOA of lisinopril?
class: ACE-inhibitor
MOA: Blocks conversion of angiotensin I to II.
Effectively decreases peripheral vasoconstriction;
also inhibit bradykinin degradation
when is lisinopril used?
HTN patients w/ DM or CHF;
post-MI tx to reduce Morbidity and Mortality
What s/e is common for lisinopril or all ACE-inhibitors for that matter?
DRY COUGH
metoprolol MOA?
selective beta-1 antagonist
when is metoprolol indicated for use?
management of acute MI
angina pectoris
heart failure
mild to moderate HTN.
May also be used to treat supraventricular and tachyarrhythmias and as prophylaxis for migraine headaches.
what is the class and MOA for metronidazole?
antibiotic, antiprotozoa medication
MOA: inhibit nucleic acid synthesis
when is metronidazole indicated for use?
C. diff -associated diarrhea and colitis** (IV)
tx of anaerobic infections and mixed infections, surgical prophylaxis requiring anaerobic coverage
H. pylori infection and duodenal ulcer disease
amebiasis caused by Entamoeba histolytica
acne rosacea (topical treatment)
Trichomonas infections.
this is a common PO medication of asthma tx, what is it’s MOA?
Montelukast
- leukotriene receptor antagonist (lipoxygenase pathway)
what is the class and MOA of mupirocin?
class - antibiotic, bactroban
MOA - inhibits protein and RNA synthesis of bacteria
Which topical antibiotic is effective against MRSA?
Mupirocin
what is the class and MOA of nitroglycerine?
class: nitrates
MOA: vasodilator
This is used as an emergency treatment for angina, MI, CHF exacerbation? How is it administered?
Nitroglycerine
- sublingually
what class is phenylephrine in and what is the MOA?
Class: sympathomimetic
MOA: selective alpha-1 receptor antagonist
when is phenylephrine contraindicated, and why?
HTN, because increases peripheral resistance (reflex bradycardia)
When is phenylephrine used?
mydriatic, dilates pupil
nasal decongestant
HEMORRHOIDS (Prep-H)
T/F
“Surgery, radiation, and chemotherapy are not mutually exclusive.”
T
Radiation and surgery are first employed to determine efficacy and possible cure rate. If this is not achievable, then chemotherapy is sought.
What is the most important distinguishing factor for antineoplastic drugs to determine the difference between normal cells and cancer cells?
Rates of growth and proliferation
what is the class and MOA of propranolol?
Class - sympatholytic
MOA - non-selective beta 1 and 2 antagonist
anti-HTN
What is a C/I of propranolol we need to be aware of?
DO NOT use in ASTHMA or DIABETICS
- non-selective; can exacerbate
what is the class and MOA of quinidine? What is a major possible side-effect of this drug?
class 1a anti-arrhythmic - Na channel blocker (limits activity and propagation in Purkinje fibers)
SE: prolonged QT
This drug is prescribed to treat arrhythmia (Ventricular), A-Fib and A-flutter, as well as Malaria..
Quinidine
this is a potassium sparing diuretic that acts by antagonism of aldosterone in the distal renal tubules
Spironolactone
- Aldosterone retains sodium and water, while increasing K+ excretion, this is blocked.
- increases Na and H2O excretion
what side effect of spironolactone should be considered in men?
gynecomastia
this is a bacterioSTATIC antibacterial agent that interferes with folic acid synthesis in susceptible bacteria, what is it and what class of antibiotics is it in?
Sulfamethoxazole
sulfonamide drug
anti-metabolite - folic acid inhibitor
(competes w/ para-aminobenzoic acid (PABA) for binding to dihydropteroate synthetase (dihydrofolate synthetase))
when telling a patient how to take sulfamethoxazole, what do you need to remember?
Do not take calcium, aluminium, magnesium or iron supplements within 2 hours of taking this medication.
Take on empty stomach: 1 hour before or 2 hours after meals.
Take with a full glass of water.
This antibiotic drug class causes tooth discoloration in children due to its high binding capacity for calcium.
What is it’s MOA? What’s an example antibiotic from this class?
tetracyclines
(fluoroquinolones also bind Ca)
- bind 30S ribosomal subunit, inhibiting protein synthesis. BacterioSTATIC
- Doxycycline
This PO treatment for asthma, though rarely used, acts similar to a stimulant, like caffeine in its ability to stimulate CNS while simultaneously causing broncho-dilation - what does it inhibit?
theophylline
- phosphodiesterase inhibitor
this drug is a pyrimidine analogue, it disrupts folate synthesis by inhibition of dihydrofolate reductase blocking DNA replication. This drug, therefore, exhibits bactericidal activity.
Trimethoprim
This drug combination is commonly used to treat the following issues:
- COMMUNITY ACQUIRED-MRSA*
- Acute Otitis Media
- Pneumonia, Pneumocystis
- Uncomplicated Urinary Tract Infections
Sulfamethoxazole-Trimethoprim
- targets TWO steps in folate synthesis when combined. making the combination, bacteriCIDAL
- can also be used as an anti-malaria combination
This antibiotic is administered P.O. ONLY for C.DIFF infection, and IV for what?
vancomycin
IV for MRSA*
What is the MOA for vancomycin?
inhibition of cell-wall biosynthesis
higher doses of this drug can be effective against varicella, which drug is it?
acyclovir
what kind of vaccine is the varicella vaccine?
live-attenuated virus
the anti-protozoa, damages parasitic DNA and inactivates plasmodium’s enzymatic ability to polymerize heme, in doing this, it allows soluble heme to stick around, which is toxic to parasites - which drug is this and which parasite is it most active against prophylactically?
chloroquine
- anti-malaria
these drug can cause severe hemolysis in individuals with G6P deficiency
chloroquine
metronidazole
this antibiotic, antiprotozoal binds to these buggers DNA, effectively halting cell division. It’s highly lipid soluble, and has a METALLIC taste - which drug is this and what MUST be avoided when using this drug?
metronidazole
- AVOID ALCOHOL - inhibits aldehyde dehydrogenase enzyme **
- tx for amebiasis
-azole antimycotic agents are among the most commonly used, what do they inhibit?
ergosterol synthesis
this chewable anti-parasitic medication is the MOST COMMONLY used of all the anti-helminthic agents, it works by destroying microtubules and it’s effective without many adverse effects - which drug is this? what does it gen. treat?
Mebendazole
- helminths! pinworms, tapeworms.
this anti-parasitic intensifies release of GABA transmission, while it’s an anti-helminthic, it also is an anti-ectoparasitic which means, it’s effective against: lice, scabies and fleas. Which drug is this? and which drugs need to be avoided during it’s use?
Ivermectin
- avoid benzodiazepines and barbiturates
- also avoid during pregnancy
which species is responsible for MOST malarial infections?
Plasmodium falciparum
malaria causes the most deaths, globally - mostly young children of Sub-Sahara Africa
Most individuals in the US who contract malaria have travelled where?
Sub-Sahara Africa or
South Asia
There are four groups of protozoa that are infectious to humans, what are these groups?
Sarcodina – the ameba, e.g. Entamoeba
Mastigophora – the flagellates, e.g. Giardia, Leishmania
Ciliophora – the ciliates, e.g. Balantidium
Sporozoa – organisms whose adult stage is not motile e.g. Plasmodium, Cryptosporidium
What are the 5 Neglected Parasitic Infections (NPIs)?
Chagas disease Cysticerosis Toxocariasis Toxoplasmosis Trichomoniasis
-typically associated with poor, marginalized, low-income communities
What is the most common, non-viral STI?
trichomoniasis
this is a parasitic infection that humans contract from cat feces or infected meats/tissues.
Humans may have swelling of lymph nodes, but gen asx. What is it?
that tell you about the organism?) (Why would that be?)
Toxoplasmosis
- only treated in immunocompromised*
Toxoplasmosis can be prevented, but not treated with ____?
Sulfamethoxazole-Trimethoprim (Bactrim)
When treatment is pursued drugs include selected antimalarial and antibiotic drugs.
this disease, spread by the kissing bug generally exhibits a swollen eye and if chronic, can cause fatal cardiopathies
chagas disease
what is the objected of chemotherapeutic drugs?
The objective of their use is to “level the playing field” so that the body’s own defense mechanisms will have an opportunity to prevail against the invaders.
Antineoplastic drugs may distinguish cancer cells from normal cells based on these 3 characteristics, which is most common?
- Rate of growth and proliferation (MC)**
- Consumption of selected nutrients
- Consumption of oxygen
- small margin of safety - these distinctions are often, imprecise
Normal cells that proliferate rapidly and consume large amounts of nutrients and oxygen are victimized by anti-neoplastic agents - what are these 5 tissues?
- Bone Marrow Cells (anemia, leukopenia, infections)
- Hair Follicles (alopecia)
- Buccal mucosa (stomatitis)
- Gonads (impotence)
- Embryonic tissues (teratogenicity)
when is someone said to be “cured” of cancer?
cancer free x 5 years
- If a cure is not attainable, the treatment goal becomes palliation and increased longevity
Why is surgery preferred for some cancer treatments?
Reducing tumor burden through surgery or radiation often causes remaining cancer cells to enter proliferation stages where they are more susceptible to antineoplastic drugs.
Most cancer drugs are administered how?
IV - optimize concentration
what is primary tumor resistance? what cancers are commonly susceptible to this type of resistance?
Primary resistance is the absence of response on first exposure to contemporary antineoplastic drugs among specific cancers. (Possibly due to absence of suppressor gene in certain cancers)
- Malignant melanoma
- Brain cancer
- Renal cell cancer
what is acquired tumor resistance?
Acquired resistance develops in response to repeated exposure to selected antineoplastic drugs. (Various mechanisms)
-Cancer cell mutations mitigate drug effects -Enhance drug efflux via P-glycoprotein**
these are common side effects caused by debris from dead cancer cells in treating leukemia and lymphoma with anti-neoplastics
tumor lysis syndrome
-Referred to as Spontaneous Tumor Lysis Syndrome if not precipitated by antineoplastics
This anti-neoplastic is an alkylating agent, what is it’s MOA?
cyclophosphamide
- inhibits DNA replication, RNA transcription and nucleic acid function
This anti-neoplastic is an alkylating agent, what is it’s MOA?
cyclophosphamide
- inhibits DNA replication, RNA transcription and nucleic acid function
How is cyclophosphamide administered?
orally - few anti-neoplastic are administered in this manner
This anti-neoplastic is an anti-metabolite agent, though it could also be considered an immunosuppressant or DMARD - which drug is it and what enzyme does it inhibit?
methotrexate
- folic acid inhibitor
- inhibits dihydrofolate reductase
Do humans manufacture their own folate?
NO
- that’s why folic acid inhibitors are bad-to-the-bone AWESOME in antibiotic/anti-neoplastics! ;) I mean, in pharm world.
this drug masquerades as a purine or pyrimidine - which become the building blocks of DNA, preventing these substances incorporation into DNA during the “S” phase (of the cell cycle), stopping normal development and division.
Methyltrexate
what are the bogus purines that methyltrexate create?
6-mercaptopurine
thioguanine
this antineoplastic, antibiotic-like, anthracycline agent is the MOST efficacious for broad range of cancers, however, cardiotoxicity limits it’s usefulness
doxorubicin
Which drug must be administered RAPID IV, for fear tissue necrosis at site of injection will occur
doxorubicin
This drug can create red urine due to a pigment in the drug
doxorubicin
this anti-neoplastic, microtubule inhibitor - reversibly binds the microtubule, and prevents cell division - which drug is it?
paclitaxel
- (S/E) can cause joint pain, sore throat and alopecia
this is an anti-neoplastic, it’s a selective competitive antagonist to breast tissue, yet partial AGONIST of uterine tissue - what is it and what is it’s MOA?
Tamoxifen
- binds E receptor and prevents RNA synthesis
what is the standard treatment for early breast cancer?
Tamoxifen
Preparation H label says, “shrinks swollen hemorrhoid tissue” what is the active ingredient and what is the MOA?
phenylephrine
- alpha 1 agonist (sympathomimetic)
SE - HTN
Will propranolol or atenolol (beta blockers), produce reflex tachycardia? why or why not?
No.
Because block B1 receptors
- otherwise BP drop would stimulate baroreceptors to activate B1.
what is a natural vasodilator? vasoconstrictor?
NO - dilates
Angiotensin II - constricts
What is the most common parasite infection?
worms
