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171 Cards in this Set

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Calcineurin inhibitors are (immunosuppressive/immune stimulating) and include _
Immunosuppressive

cyclosporine, tacrolimus, sirolimus
Biggest side effect is nephrotoxicity
Mycofenolate mofetil and Azathioprine are considered _
anitproliferative/antimetabolic agents
MC cytotoxic drug?
Cyclophosphamide

SE?
hemorrhagic cystitis
Classic example of immune modulating biologic agent?
Anti- IL2R mAbs - Daclizuman, Basiliximan
block IL2 mediated T cell activation
All biologics have an increased risk of _
infection and cancer
Major side effect of CD-3 therapy is _
cytokine release syndrome

typically begins 30 min after treatment

causes high fever, chills, HA, rigor, htn, N/V/D

can also cause pulmonary edema, ARDS, cardiac arrest

How can cytokine release be prevented?
administration of glucocorticoids before the injection on CD3
Cyclosporine binds to _
Tacrolimus binds to _

Both of these are considered _
cyclophilin
FKBP (and cyclophilin - more potent)

calcineurin inhibitors - they inhibit the transcription of IL2
MOA of Sirolimus
blocks downstream signlaing through TCR and inhibits proliferation

Does NOT block IL2 (despite being considered a calcineurin inhibitor - it actually isn't)

SE?
myelosuppression
DoC for ITP?
Prednisone
DoC for autoimmune hemolytic anemia?
Prednisone
DoC for AGN?
Prednisone
Binds to both TNF alpha and TNF beta?
Etanercept -

used in arthritis
Binds to TNF alpha and suppresses inflammatory cytokines IL1 and IL6
Infliximab

(also adalimumab)
Inhibits T cell Costimulation by blocking secondary binding of CD80/86 (APC) with CD 28 (TC)
Abatacept
Treatment of MS?
INFbeta 1-a and INF beta 1b

And what if the patient becomes refractory to INFb?
Glatiramer acetate

or Mitoxantrone
Use of Levamizole?
Colorectal cancer

se?
severe agranulocytosis
Treatment of multiple myeloma?
Thalidomide

inhibits TNFa and angiogenesis
Nonspecific adjucant or immunostimulant used in bladder cancer
Bacillus Calmette Guerin (BCG)
Tx of chronic granulomatous disease?
INF gamma
Approved in treatment of several neoplasma such as hairy cell leukemia, HTLV, CML, malignant melanoma, Kaposi's sarcoma, Hep B and C
INF alpha
Binds to CD20 triggering complement mediated lysis of the cell
Rituximab

uses
follicular B cell or non Hodgkin;s lymphoma
Binds to GPIIb/IIIa receptor on activated platelets, preventing aggregation.
Abciximab
Tx of OD of acetominophen?
Charcoal, Nacetylcysteine (supplies sulfhydryl groups that replete glutathione)
Calcium oxalate crystalluria is a/w _
ethylene glycol ingestion (antifreeze)
Treatment of organiophosphates exposure? (Ie a farmer wearing short sleeves)
atropine for sx

pralidoxime (2-PAM) breaks covalent bond
Treatment of lead poisoning? (seizures, abdominal cramping, anemia, hepatitis,)
EDTA (chilation) + dimecaprol
Tx of Arsenic poisoning? (garlic breath, rice water stools)
Dimecaprol
Treatment of Iron OD?
deferoxamine mesylate
Treatment of CN poisoning?
sodium nitrite, sodium thiosulfate
Sustained rapid eye mvmnt, confusion, euphoria, clumsiness, overreaction of reflexes, relaxation of jaws & ankles is indicative of
serotonin syndrome

how do you antagonize?
Cyproheptadine!
-specific 5HT2 antagonist
You should NOT administer charcoal or induce emesis with _ ingestion.
corrosives (acids and alkalines)

what should you do?
dilute with milk or water
Antivenom for snack bite?
crotaline polyvalent fab
What drugs are known for their side effects of cytokine release syndrome 30 min post transfusion? (fever, chills, NVD, arthralgias, and fatigue)?
Muromonab CD3 Ab

Use and MOA?
Acute organ transplant rejection

decreases T cells by cell death and also by T cell margination to vascular endothelial wall
MOA of Daclizumab and Basiliximab?
Bind IL-2 receptors, blocking binding from activated lymphocytes
Calcineurin Inhibitors Include _ , what is there MOA?
Cyclosporin, Tacrolimus, Sirolimus

C: binds cyclophilin, T: binds cyclophilin and FKBP, S: blocks FKBP. Ultimately inhibits transcription of IL2
MOA of mycophenolate mofetil?
inhibits de novo synthesis of purines

Use?
Steroid refractory GVHD, solid organ transplant
Azathioprine MOA?
Prototypical Antimetabolite, Gets metabolically activated interferes with purine metabolic and lymphoid cell proliferation.


Use ?
Dose should be reduced if the patient is on what other drug?
Renal allografts, actue GN,

Allopurinol (needs xanthine oxidase)
What drug causes hemorrhagic cystitis?
Cyclophosphamide
MOA of Vincristine?
prevents mast cell degraulation, binds microtubules in cells preventing the release of histamine

Use?
ITP refractory to prednisone
MOA of Infliximab?
binds TNF a, suppression of downstream cytokines
Used in crohn's, RA
MOA of Etanercept?
binds both TNFa and TNFb,
Used in RA and psoriatic arthritis
MOA of adalimumab?
blocks interaction of TNF with TNF receptors - similar to infliximab
MOA of Abatacept?
binds CD80/86 on APC and inhibits T cell activation and cytokine release

Use?
RA

How do you treat MS?
INF beta (interferes with T cell adhesion to endothelium)

and if that doesn't work?
Glatiramer acetate, or Mitoxantrone
Levamisole is an immuno(depleting/stimulating) drug
stimulating, activates macrophages

Use
colorectal cancer
MOA of Thalidomide?
Inhibits TNFa and angiogenesisis, reduces phagocytosis by neutrophils and increases production of IL-10.

Use?
Mutltiple Myeloma, erythema nodosum
What is IFNy used for?
Chronic granulomatous disease

SE?
fever, flu sx, anorexia, fatigue, malaise (all cytokines share these SE)
What is GMCSF used for?
pre term neonates and neutropenic patients, to help them fight infections
What is IL2 used for?
metastatic renal cell carcinoma and malignant melanoma

SE?
fever, flu sx, anorexia, fatigue, malaise

All cytokines share these side effects
Trastuzamab MOA and use?
Binds her-2/neu in breast cancer
MOA of Rituximab?
Binds CD20 on B lymphocytes,

Use?
B cell or non-hodgkins lymphoma
MOA of Abciximab?
binds GP IIb/IIIa receptor on platelets, preventing aggregation

Used as an adjunct to heparin
What are the 4 main mechanisms of acne?
1) hyperkeratinization- inc in loose cells in follicle, responsive to androgens
2) sebum production- responsive to androgens
3) bacterial component- P. acnes- G+ anaerobic rod; produces lipasesform FFA from sebum
4) inflammatory- irritation from FFA, immune response to P. acnes
What mechanism of acne production does salicylic acid target?
Specifically it is Keratolytic

(it decreases coryneocyte adhesion
What mechanisms of acne production does Azelic Acid target?
Inflammation (oxygen free radical scavenger), antibacterial ( inhibits thioredoxin reductase), and keratolytic

Side effects?
Hypopigmentation
Which has more mild side effects. 1st, 2nd, or 3rd generation retinoid receptors?
3rd generation, interact with fewer retinoid receptors allowing for a milder side effect profile
What mechanism of acne production do retinoids target?
keratolytic (they increase mitosis, increasing turnover and decreasing cell adhesion), lower inflammation

SE?
appearance of worsening acne, takes of the top layer of skin and exposes all the acne that hadn't made its way up get, anti wrinkle, yields pink smooth skin
What mechanisms of acne production are targets by oral isoretinoin?
(accutane) All 4!
Keratolytic
Antibiotic
Antiinflammatory
Decrease Sebum production

SE?
inflammatory bowel disease
Erythromycin when given for acne is given (orally/topically/both)
both

MOA?
Inhibits 50s RNA inhibiting translation
Clindamycin when given for acne is given (orally/topically/both)
both

MOA
binds 50s ribosome, (different site than erythromycin)
Tetracycline when given for acne is given (orally/topically/both)
both

MOA?
binds 30 s ribosomal subunit, inhibits Elongation

SE include photosensitivity (worse with dairy), tooth and bone effects,
Minocycline when given for acne is given (orally/topically/both)
orally

MOA?
its a tetracycline which inhibits elongation by binding 30s
Used in moderate to severe chronic plaque psoriasis and acts my reducing active T cells involved in psoriasis leaving other T cells largely unaffected
Alefacept
What drug inhibits dihydrofolate reductase?
Methotrexate (used in RA, transplants, and psoriasis)

Ultimately it decreases IL-1
Which is more likely to lead to skin cancer? UVB or PUVA?
PUVA - it has a longer wavelength and therefore is a lot stronger
Where is the reward system?
ventral tegmental area
facilitates action of GABA and inhibits activation of NMDA receptors
alcohol
Patient with history of alcohol abuse presents with memory loss, dementia, anterograde amnesia, confabulation. What's this called?
Korsakoff syndrome
How do you treat alcohol addiction?
disulfiram - inhibits acetaldehyde dehydrogenase - causes an adverse rxn when the patient drinks, they get really sick to stomach

For maintenance?
Acamprosate - lowers activity of receptors for glutamate

A - without +(pro) Camp ate - glutamate
Without glutamate receptors, which are Gs so they trigger and increase in cAMP
How do you treat alcohol withdrawal?
Propanolol for tremors, and reduction of HR and BP

Benzos to prevent delirium and seizures
Blocks dopamine transporter, blocks NE and 5-HT reuptake
cocaine
What is an adverse drug event?
any drug related incident that causes harm to the patient (doesn't mean there was an error)
Ex: patient has seizure, is given a benzo. When they wake up they stand up and fall down

Risk factors?
polypharmacy, multiple prescribers, age, female gender, cognitive impairment, prior adverse drug rxns
What is a drug error?
inappropriate or incorrect omission of drug, even if it doesn't cause harm
"Lead pipe" muscle rigidity, autonomic dysregulation, hyperthermia, and altered mental status are signs of what condition?
Neuroleptic Malignant Syndrome - due to dopaminergic antagonist (onset within days to weeks)

How do you treat this?`
BZD (mild)
Dopamineric agonist - Bromocriptine (if moderate)
Dantrolene (severe)
Elevated temperature, increased pulse, increased blood pressure, constricted pupils, hyperactive bowel sounds are all signs of what condition?
Serotonin syndrome caused by serotoniergic drugs (opioids, SSRIs) - onset within minutes to hours
MOA of mycophenolate mofetil?
Inhibits de novo synthesis of purines, thus inhibits B and T lymphocytes ( acts on inosine monophosphate dehydrogenase)
 Selectively targets Inosine monophosphate dehydrogenase, which is required to make IMP (the first purine) de novo. Lymphocytes (unlike other rapidly proliferating cells) RELY solely on the de novo synthesis of purines as opposed to the salvage pathway. As such, this drug specifically targets LYMPHOCYTES.

Use?
Refractory rejection and GVHD (steroid resistant)
How do you treat ITP refractory to prednisone?
Vincristine
MOA of methotrexate?
interferes with thymidine synthesis --> blocks DNA synthesis

(specifically inhibits dihydrofolate reductase)
How should you approach patients who are likely to have a rejection to a transplant (for instance, those with high levels of anti-HLA abs)?
Plasmapheresis every other day, modify humoral rejection mediated by B cells

IV immunoglobulin - to suppress Ab production
Maintenance therapy consists of
calcineurin inhibitor, GCs, and an antimetabolite
Infliximab binds _
TNFa (which suppresses IL1, IL5, and adhesion molecules involved in leukocyte activation and migration)

Used in
crohns and RA

CI in CHF patients
Treatment of follicular B cell or non Hodgkins lymphoma?
CD20
Alefacept is used for
Psoriasis
What drug is notorious for delayed toxicity?
Amiodarone
90% of Acetominophen is metabolized via _ with _ or _
hepatic conjugation with sulfate or glucoronide

5 % does P450 oxidation and produces _
N-acetyl para benzoquinonemine (NAPQI) , which then reacts with glutathione (GSH) to form an inactive product.

If is NAPQI that destroys hepatocytes and renal tubular cells. GSH depletion --> excess NAPQI and hepatotoxicity!!! Thus why antidote to acetominophen OD is N acetyl cysteine - it repletes the glutathione
What toxicity can cause irreversible blindness?
methanol (--> formic acid)
- found in paint thinners, wood strippers
How do you treat?
Fomepizole (antidote) - competes with Alcohol dehydrogenase

then Leucovorin q 4 hours x 6

if that's not available give them ethanol (competes with AD)
How do you treat a patient who ingested a bunch of antifreeze?
Specific antidote = Fomepizole, competes with AD

Then... pyridoxine (100mg) + thiamine (100 mg) IV daily

If that's not available, then give them Ethanol!!!
MOA of pralidoxime? What is it used for ?
Used for tx of organophosphate poisoning.

Breaks the covalent bond between the organophosphates and acetylcholinesterase
Patient presents with htn, tachycardia, fever, dry mouth, dry eyes, urinary retention, hallucinations, and confusion. What does this look like, and how do you treat?
(dry as a bone, hot as a pistol, blind as a bat, mad as a hatter) --> Anticholinergic OD

Treat with Physostigmine
Patient presents with hypotension, abdominal pain, N/V, convulsions, delirium. You find out that he is a landscaper and spend all day spraying insecticides. How do you treat?
(Arsenic poisoning)

Endotracheal tube if unstable, IV fluids, gastric lavage, DIMECAPROL,

If it was organophosphate poisoning - such as parathion, malathion also seen in insecticides and the pt has DUMBBLESS how would you treat?
Atropine to control sx, 2 pralidoxine to regenerate the AchE
What is the urinary metabolite of cocaine?
benzoylecgonine
Which acne medication has a se of the appearance of worsening acne?
Tretinoin - it is exfoliative, increases mitosis, increasing cell turnover. It takes off the top layer of skin and exposes all the acne that hasn't come to the surface yet.

At what time of the day is this applied and why
Night time, because the compound degrades in UV light, so side effects are worse
_ is converted to it's active form by esterases in the skin
Tazarotene

binds RARs, and is keratolytic and has anti-inflammatory
The one acne medication that targets all four of the abnormalities found in acne?
Isotretinoin

sideeffects?
super teratogenic, - 2 forms of birth control,

dry skin, peeling, dry eyes, nosebleeds, alopecia.

Interacts with tetracyclines and can cause pseudotumor cerebri
Hormone based therapy for acne?
ethinyl estradiol and norgestimate
increases sex hormone binding globulin and decreases free testosterone. Decreases sebum production, and decreases hyperkeratinization.

Used for moderate inflammatory acne in females
What schedule has the highest abuse risk, and has no safe medical use in US?
Schedule 1 (C-1)

This includes heroin, marijuana, LSD, PCP, cocaine
What are some example of Schedule II drugs?
(high abuse risk, but have a safe and accepted med use) includes Morphine, oxycodone, dextroamphetamine
What are examples of schedule III drugs?
(accepted med use)

Acetominophen/Codeine - Vicodin
Examples of Schedule IV drugs?
Diazepam, phenobarbital, darvocet
Schedule V drugs?
involve preps containing limited quantities of certain stimulant or narcotic drugs
Every practitioner who prescribes controlled substances must register with _ and _
DEA and DPS
- exemptions: all of the following may prescribe CIII-CV drugs if acting in the course of employment for a DEA registered hospital
• Interns or residents
• Physicians on staff at VA hospital
• Individual practitioner
When do CIII-IV drugs expire?
6 mo from date of issue
When do CII drugs expire?
7 days after issue

require an official rx form or triplicate
Contents of a Prescription?
Date, Patient Name and Address, DOB (not required), Drug (brand vs generic), Name of Drug (w/o abbreviation), Strength (concentration AND dose), Quantity, Directions for use, Practicioner's name address and phone #, Refills,
Sig
directions to the pt that you want to be printed on the prescription bottle.
abbreviation for drop or drops
gtt (s)

both eyes, left eye, right eye?
o.u.
o.s
o.d (dexter)
abbreviation for

three times a day
tid

four times a day?
qid
What does qid stand for?
four x a day

qhs?
once at bedtime
Abb for 'every other day'?
qod - but DONT use this, write it out!!!

qod gets confused
abb for microgram?
mcg (NOT ug) -

don't confuse with mg - milligram
Abb for three times a week?
TIW - DON"T USE, write it out!!
Abb for subcutaneous?
sub-Q (NOT sc or sq)
Where is the DA reward pathway?
Ventral Tegmental Area
At what blood alcohol level will someone experience impaired motor function, ataxia, slurred speech?
100-200 mg / dL
What drug used in the treatment of alcoholism causes severe ha, n, and v when combined with small amounts of alcohol?
Disulfiram - inhibits acetaldehyde dehydrogenase

these patients will have adverse rxns when they consume alcohol
Which drug used in the treatment of alcoholism decreases the craving for alcohol and is therefore used to maintain abstinence?
Acamprosate (decreases activity of receptors for glutamate)
What drugs are used to treat acute alcohol withdrawal?
BZDs - to prevent delirium or seizures

Propanolol - to decrease tremors, HR and BP -- remember this is the only beta blocker that is highly lipophilic and gets into the CNS
What illegal drug when ingested can cause severe bowel gangrene?
Cocaine
What illegal drug stimulates pre and post synaptic 5HT receptors?
LSD (hallucinogenic)
What illegal drug blocks NMDA type glutamate receptors in cortex and limbic structures, slowing down excitation in brain causing distorted perceptions of sight and sound, producing an "out of body" experience?
PCP and ketamine
How do you treat opioid withdrawal?
Methadone (for short or long term detox)

for initial treatment: Buprenoprhine

For maintenance treatment: Buprenorphine + Naloxone
How do you treat quinidine overdose (GI disorder, tinnitus and deafness; usually a patient on a heart drug takes an OTC antacid)?
Acidify the urine by giving them cranberry juice or vitamin C
If the patient develops anuria, and you need to increase urinary output without changing electrolytes, which diuretic do you use?
Mannitol!
What antidote contains sulfhydryl groups and what do they do?
N -acetyl cystein,

replete Glutathione!!! (conjugates NAPQI to make it nontoxic and excretable by the kidneys)
Fomepizole is used for
antidote for Ethylene glycol or methanol poisoning

If this is not available, what should you give the pt?
Ethanol!

competition for alcohol dehydrogenase
A farmer who was working all day in his tank top comes in complaining of diarrhea, frequent urination, sweating, and watery eyes. PE shows he is bradycardic, and has excessive salivation and lacrimation. Dx and Tx to control symptoms?
organophosphate exposure - parathion, malathion - in insecticides


Atropine controls symptoms
What if you wanted to regenerate the Acetylcholinesterase?
2-Pralidoxime!
A patient OD's on her TCA she's taking for depression while being high on mushrooms. She presents with tachycardia, confusion, elevated temperature. How do you treat?
OD on anticholinergics, treat with Physostigmine!
If you see rice water stools and garlic breath in the vignette, what are they talking about?
Arsenic exposure

how do you treat?
dimecaprol
A painter presents with seizures,abdominal cramping, neuropathy, and fatigue. Lab shows he is anemic. How do you treat the seizures?

How would you treat if he had increased intracranial pressure?
(lead poisoning)
Diazepam - for seizures
Mannitol - for increased ICP

What is the specific antidote for lead poisoning?
Dimecaprol + EDTA
Parents bring their child in who is in who has nausea, vomiting, and diarrhea with bloody stools. They believe she ate her mom's prenatal pills that were on the counter. How do you tx?
(Iron overdose)

Deferoxamine!
A patient presents to the ER with a bp of 210/130 and is infused with a nitrate to relax the blood vessels. He presents 24 hours later with a headache, generalized confusion, bizarre behavior, and shortness of breath. Shortly after his arrival he has a seizure. What is the dx and tx?
(Sodium Nitroprusside was given to the patient --> cyanide poisoning )

Treat with Sodium nitrate and sodium thiosulfate (N promotes formation of methemoglobin - cyanide binds to it, T breaks bond and forms the less toxic cyan ion which can be excreted)

What if IV access is unavaiable right away?
hold amyl nitrite pearls under nose (assuming the patient is spontaneously breathing)
confused, psychotic episodes, DAMAGED nasal septum, running of nose, what should you NOT give this patient?
A beta blocker - You will cause signif alpha-adrenergic overdrive

If necessary, give one dose benzodiazepine

(This is Cocaine)
The ideal drug for older adults undergoes _
Phase II metabolism (doesn't change much with age)
best predictor of an anticoagulant response?
age
Lead pipe muscle rigidity, hypertension, hyperthermia and altered mental status are sx of ...

How do you treat?
Neuroleptic Malignant Syndrome

Mild: benzo, Moderate: bromocriptine (da agonist), Severe: dantrolene - for mm rigidity

What meds should you use in the future for this patient?
Atypical antipsychotics
-questiaptine/seroquel
Muscle dystonia, hypertension, hyperthermia and altered mental status are sx of ...
Baclofen withdrawal (mm relaxant) looks a lot like NMS except dystonic instead of rigid

this is life threatening
Volume of distribution =
TD (total drug dose)/Plasma Concentration
Infants typically require a (larger/smaller) loading dose for lipophilic drugs and a (larger/smaller) loading dose for hydrophillic drugs
Smaller

Larger

(remember babies have more water...also remember that highly lipid soluble meds are deposited in breast milk)
Why does chloramphenicol cause gray baby syndrome?
baby's have decreased metabolism by glucuronyltransferases
What metabolism pathway is well developed in infants?

What pathway(s) are delayed up to 1 year?
Sulfation is well developed

glucuronidation and oxidation is delayed

What about elimination??
Toddlers may have shorter elimination half lives due to increased renal elimination

----think about it, toddlers are peeing all the time
If quinolones are given to a patient younger than one year, they may cause...
permanent lesions in the cartilage of weight bearing joints, and reversible arthralgia
The facial abnormalities seen in fetal alcohol syndrome are a/w heavy consumption of alcohol during what part of the pregnancy?
first trimester
Decreased appetite, mental alertness, increased heart rate, increased BP, increased temperature, and dilated pupils are signs that someone is under the influence of _
cocaine
Rapid emotional swings can be produced by what class of addictive drugs?
hallucinogens - LSD, Mescaline, Psilocybin

stimulation of presynaptic and postsynaptic serotonin receptors
Pupillary dilation, increased BP, pulse, flushing salivation, lacrimation, hyperreflexia, prominent visual effects, intense color are signs of what illegal drug?
LSD
Intoxication of benzodiazepines is managed with ....
Flumazenil
For CIII-V prescription drugs, what do you need to know about the quantity?
Refills?
Expiration?
Quantity much be written numerically and as a number!
Limit of 5 refills within 6 months
expires in 6 months
How many refills are allowed for CII prescription drugs?
Zero
If you don't have a DEA number, in what circumstances can you still prescribe CIII-V drugs?

CII?
If you are employed at a DEA registered hospital and are interns or residents, an individual practicioner, or on staff at a VA hospital

No exceptions for CII
Mechanisms of benzoyl peroxide?
antibacterial and keratolytic
Inhibitor of thioredoxin reductase and tyrosinase
Azelaic Acid (Azelex®)

SE?
hypopigmentation
T retinoin?
increases TuRnover of cells --> keratolysis

causes appearance of worsening acne
whats different about the structure of isotretinoin? (the one that inhibits all 4 mechanisms of acne prod)
It is cis as opposed to trans
Absorption of tetracyclines is inhibited by concurrent use of _
antacids
What antibiotic used in acne treatment can cause ototoxicity and vestibular effects?
minocycline
Acitretin MOA
normalizes proliferation of keratinocytes (psoriasis)
Tx of Beta blocker OD?
glucagon - to increase inotropy of heart
Tx of Digitalis OD?
Anti-digitalis Fab fragments
Tx of copper poisoning?
penicillamine

(this is also treatment
Tx of TCA overdose?
IV NaHCO3
Tx of heparin toxicity?
Protamine

Tx of Warfarin OD?
Vitamin K, fresh frozen plasma (contains factors II, VII, IX, X protein C and protein S)
-afil
Erectile dysfunction
ie Sildenafil
-ane
Inhalational general anesthetic (halothane)
-azepam
-zolam
Benzodiazepine
-azine
Phenthiazine (neuoroleptic, antiemetic)

- Chlorpromazine
-azole
antifungal
-etine
SSRIs
-oxin
cardiac glycoside
-pril
ACE inhibitor
-triptan
5 HT agonists (migraines)
-tidine
H2 antagonist

cimetidine