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Drugs
Maryland Path1 Drugs
105
Biology
Graduate
11/24/2009

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Term
Need to stimulate bladder emptying or pupil constriction.  You would use this class of drugs:
Definition

Cholinergic agonists

 

Muscarinic agonists,specifically

 

Like ACh, Bethenacol (bladder) or Pilocarpine

Term
Need to stimulate nicotinic receptors in the eye, and will not be affected by Acetyl-cholinesterase inhibitors.  Use...
Definition

Carbamylcholine

 

Cholinergic agonist (Nicotinic > Muscarinic)

Term
Need to stimulate muscarinic receptors in GI tract, bladder and eye that is unaffected by  Acetylcholinesterase inhibitors.  Like for bladder tone, use...
Definition
Bethenacol
Term
Need something that will cross the BBB to contstric the pupil and treat glaucoma.  Topical use of...
Definition
Pilocarpine
Term
Need to block ACh secretion at presynatpic terminal of neuromuscular junctions (skeletal muscle).  Use a muscle relaxant called...
Definition

Botulinum Toxin

 

botulinumtoxinA inhibits SNAP-25

botulinumtoxinB inhibits VAMP

Term
Don't want to block Ca++ transport at NMJ presynaptic terminal in a pateint with existing neuromuscular problems. Avoid...
Definition

aminoglycosides and other antibiotics!

Avoid -CINs and -cyclines

 

Amikacin, gentamicin, kanamycin, neomycin, tetracycline, doxycycline

Term
Best way of blocking NMJ transmission -- muscle relaxant.  use:
Definition
nAChR antagonists (post synapse effect)
Term
Need to relax skeletal muscle for someone who has just come in for trauma and likely has vital organ failure.  Use:
Definition

Atracurium

 

non-depolarizing, competitive nAChR antagonist

Term
Need a quick acting muscle relaxant that does NOT cause histamine release
Definition

Mivacurium

 

Non-depolarizing, competitive nAChR inhibitor

Term
Need a fast-acting muscle relaxant, but must avoid this in ppl with history of malignant hyperthermia/burns/trauma
Definition

Succinylcholine (SuCh)

 

depolarizing, non-competitive nAChR inhibitor

Term
The grandfather of non-depolarizing muscle relaxants with long onset of action and very long duration of action
Definition
Pancuronium
Term
Need an M1 receptor selective antagonist that can help treat intestinal hypermotility and diarrhea by reducing glandular secretions.  Use:
Definition
Pernzapine
Term
Need to treat Parkinson's disease with this M1-receptor selective antagonist that crosses the BBB.  Use:
Definition
Trihexyphenidyl (use with Benztropine -- nonselective)
Term
Need to selectively inhibit urinary bladder tone to treat incontinence.  Use:
Definition

Darifenacin or Tolterodine

(M3R selective antagonists)

Term
The prototype drug to use to inhibit parasympathetic outflow in the body.  Use to avoid cholinergic crisis, but beware!  it causes cardiace and CNS effects b/c it is uncharged and can cross the BBB:
Definition
Atropine
Term
Need a drug that will treat Parkinson's disease by treating the cholinergic imbalance, that is also non-selective its cholinergic receptor preference.  Use:
Definition

Benzotropine (along with Trihexyphenidryl)

 

non-selective muscarinic receptor blocker

Term
Need to dilate eyes for longer time period than just 6 hrs.  Use:
Definition

Cyclopentolate

 

non-selective muscarinic receptor antagonist

Term
Need to relax muscles and reduce secretions during intubation.  and want something with less CNS/cardiac effects.  Also need to prevent vagal reflexes (cholinergic crisis) post surgery.  Use:
Definition

Glyccopyrrolate

 

non-specific muscarinic receptor antagonist

good for use in GI/GU tracts

Term
Need prophylaxis for motion sickness that will penetrate skin readily for topical treatent
Definition
Scopolamine
Term
Need to dilate eyes for an eye exam.  Want the effect to wear off within 6 hrs.  Use:
Definition

Tropicamide

 

non-selective muscarinic receptor antagonist

Term
Need to treat symptoms of chronic bronchitis or emphysema by bronchodilation without any effect on viscosity.  Use:
Definition

Tiotropium

 

M1/M3 selective muscarinic receptor antagonist

Term
Need some relief of symptoms caused by respiratory tract diseases (cold, chronic rhinitis, chronic bronchitis and emphysema) that can be used in conjuction with beta2 agonists.  Like, bronchodilation without affecting secretions.  Use:
Definition

Ipratropium

 

non-selective muscarinic receptor antagonist

Term
Need to build up ACh at synapses, but cannot give ACh.  Use:
Definition

Anticholinesterases!

 

inhibits degradation (indirect cholinomimetics)

Term
Therapeutic carbamates (anti-ChE):
Definition

neostigmine

pyridostigmine

physostigmine

Term
therapeutic anti-ChE that does not form covalent bond with ChE, so rapidly reversible and is charged:
Definition
Edrophonium
Term
Insecticides:
Definition

Malathion

Diazanon

Carbaryl

Term
Chemical warfare agents (nerve agents)
Definition

Vx

Soman

Sarin

Soman

Tabun

Term
insectiside found in gardening to get rid of bugs on plants:
Definition
carbaryl
Term
insecticisde used by pest exterminators whic does not dissociate easily
Definition
diazinon
Term
very widely used insecticied for mosquito control, sprayed over states!
Definition
Malathion
Term
Irreversible acetylcholinesterases
Definition
organophosphates, including pesticides and nerve agents (except carbaryl)
Term
When you want to increase levels of ACh in the eye to facilitate constriction (glaucoma rx), need it to penetrate the BBB.  Use:
Definition

Physostigmine

only uncharged hydrophobic anti-ChE

Term
Want to treat paralytic ileus and atony of urinary bladder (trouble voiding urine).  Use:
Definition
Neostigmine with bethanechol (synergistic action)
Term
Need to treat narrow-angle glaucoma. What would be a good anti-ChE and cholinomimetic combo?
Definition
physostigmine + pilocarpine
Term
Want to classicaly treat myasthenia gravis with a anti-ChE and anti-muscarinic (to avoid vagal reflex).  Use:
Definition
neostigmine or pyridostigmine + atropine/IV glycopyrrolate
Term
want to treat poisoining due to anti-muscarinic or anti-nicotinic (anti-PSYMP) agents.  Use:
Definition
anti-ChE agents
Term
need to recover from neuromuscular block (due to non-depolarizing agent) following surgery.  use:
Definition
neostigmine + antimuscarinic (atropine)
Term
Want to treat progressive degeneration of Alzheimer's disease.  Use:
Definition

Galantamine (so galant to save the day!)

or

Tacrine

Term
most potent nerve agent with lowest lethal dose
Definition
Vx
Term
want to reverse the effects of anti-ChE.  Use:
Definition

Pralidoxime

 

Need to act quickly with the organophosphates, before enzyme "aging"

Term
need a prophylactic treatment of nerve agent exposure.  Use:
Definition

Galantamine

or

recombinant human BuChE which acts to scavenge nerve agents (OPs)

Term
(bradycardia, miosis, diarrhea)
Definition
cholinergic crisis 
Term
Class of antineoplastic drugs that inhibit DNA synthesis by cross-linking strands
Definition

Alkylating agents

 

Cisplatin

Cyclophosphamide

Dacarbazine (in ABVD)

Melphalan

Term

alkylating agent that causes severe vomiting, and can cause hearing/vision loss

 

binds DNA and protein

Definition
Cisplatin
Term

alkylating agent, nitrogen mustard that is a prodrug that needs liver enyzmes for activation

 

part of the combination treatment: CHOP and CVP

Definition
Cyclophosphamide
Term

Triazine alykylating agent

part of combo ABVD

Definition
Dacarbazine
Term
Orally active nitrogen mustard (alkylating agent) with milder side effects
Definition
Melphalan
Term

Very potent chemoRx agents that act by 3 antineoplastic mechanisms:

production of O2 free radicals --> toxic

topoII-dep DNA cleavage

intercalate into DNA

Definition

Daunorubicin

Doxorubicin

Term
cardiotoxic and myelosuppressive antibiotics used as chemotherapeutic agents
Definition
Daunorubicin and doxorubicin
Term

antibiotic ChemoRx agent that is found in CHOP

part of treatment of AML

Definition
Doxorubicin (or hydroxyldaunorubicin)
Term
monoclonal antibody used to improve survival in non-hodgkin's lymphoma because it recognizes CD20 on B cells:
Definition
Rituximab
Term
Antibody against HER2 receptors for treatment of breast cancer
Definition
Trastuzumab
Term
antineoplastic drug class that require proliferating cells and are cell cycle phase-specific
Definition
Anti-metabolites
Term
anti-neoplastic agent that exploits unique increase amt of asparagine in tumor cells
Definition
L-Asparaginase
Term
anti-neoplastic agent that inhibits DNA methylation, a pyrimidine analog
Definition
Azacitidine
Term
inhibits pyramidine synthesis (pyrimidine analog) used in treatment of AML treatment
Definition
cytosine arabinoside (ARA-C)
Term
pyrimidine analog used to inhibid thymidilate synthesis in tumor cells
Definition
5-Fluoruracil
Term

similar to thalidomide

anti-angiogenic and immunomodulatory

Definition
Lenolidomide
Term

folic acid analog that inhibits DHF reductase

indirectly inhibits important dTMP synthesis rxn

Definition
Methotrexate
Term

purine analog (anti-metabolite) that inhibits adenosine deaminase in tumor cells

used in Rx of CLL

Definition
Pentostatin
Term
an anti-neoplastic drug that stabilized microtubule polymerization
Definition
Paclitaxel
Term

anti-neoplastic drugs that inhibit mitosis (M phase) by arresting tumor cells in metaphase

 

also part of ABVD treatment

Definition

Vinblastine (ABVD)

Vincristine

Term
hormonal antineoplastic agent that inhibits aromatase; useful in post-menopausal breast cancer
Definition
Letrozole
Term

causes selective lysis of lymphoid tumors

hormonal anti-neoplastic agent

corticosteroid

Definition
Prednisone
Term
anti-neoplastic agent that blocks Estrogen Receptors expressed in breast cancer
Definition
Tamoxifen
Term
tyrosine kinase inhibitor used in cancer treatment, specifically for CML since it targets the philly chromosome product --> bcr-abl fusion protein
Definition
Imatinib (Gleevac)
Term
Other Tyrosine kinase inhibitors that are used to treeat CML b/c of their ability to target mutated proteins
Definition

Dasatinib

Nilotinib

Term

Copper-chelating antibiotic that causes pulmonary toxicity

part of ABVD

Definition
Bleomycin
Term
proteosome inhibitor that induces apoptosis in multiple myeloma
Definition
Bortezomib
Term

inhibits ribonuclease diphopshate reductase (an enzyme imp for DNA synthesis in tumors)

used for myeloproliferative disorders (CML, AML)

Definition
Hydroxyurea
Term

part of ATRA

retinoic acid that causes cell differentiation

good for head and neck cancers, squamous cell carcinomas

 

Definition
Tretinoin
Term

used for hematological malignancies

CLL in particular (most common one)

Definition
Fludarabine
Term

adjuvant agent for melanoma

Hairy cell leukemia

Karposi's sarcoma

Definition
alpha-IFN
Term

anti-neoplastic agent that prevents angiogenesis

multiple myeloma

renal/brain cancers

teratogen

Definition
Thalidomide
Term
catecholamine that acts on all alpha and all beta receptors (except beta3), and is a sympathetic NT
Definition
epinephrine
Term

catecholamine that acts on alpha receptors and beta1 receptor (weak beta2receptor)

sympathetic NT

Definition
norepinephrine
Term
synthetic catecholamine that is a beta receptor agonist only
Definition
Isoproterenol (ISO)
Term
synthetic catecholamine that is a β1-selective agonist
Definition
Dobutamine (DO)
Term
catecholamine that is binds D1 to cause BV dilation and also is a beta1-selective agonist
Definition
dopamine (DA)
Term
stimulation of D1R with this synthetic analog of dopamine lead so maintenance of renal function -- urinary output
Definition
fenoldopam
Term

Indirect acting NE-releasers (non-catecholamine)

Use the "NE channel"

Definition

tyramine

ephedrine

amphetamine (-->ecstasy)

Term
Need a non-catecholamine agent that indirectly acts to increase NE outflow and directly stimulates beta2R in order to treat nasal decongestion.  Use:
Definition
ephedrine
Term
a non-catecholamine agent that releases NE indirectly through NE channel, but has lately gone out of fashion b/c of abuse potential (strong CNS effects)
Definition
amphetamine
Term
dietary prototype of NE-releasers (non-catecholamines that indirectly act to increase NE transmission).  When mixed with MAOIs, can lead to massive hypertensive crisis.  found in aged cheese and wine
Definition
tyramine
Term
NE/DA uptake inhibitor
Definition
cocaine
Term
need a good decongestant (constricts wollen mucous membranes, decrease secretions) and can also be used to dilate pupils.  found in Sudafed-PE.  Use:
Definition

phenylephrine

or

methoxamine

Term
an agonist of a sympathetic adrenergic receptor that actually decreases release of NE -- sympatholytic action
Definition

clonidine

 

alpha2R selective agonist

Term
an alpha adrenergic agonist that is used specifically in ophthamology -- interacts with MAOIs to produce sympathetic overdrive
Definition
Brimonidine
Term
used in management of asthma, desinged specifically to get rid of cardiac effects and increase duration of action
Definition
Albuterol and Salmeterol
Term
longest lasting asthma drug
Definition

salmeterol

 

beta2 selective agonist

Term
Need something that will prevent preterm labor through IV in the hospital.  But watch out!  Is associated with pulmonary edema! Use:
Definition

Ritodrine

 

beta2 selective agonist

(relaxes uterus)

Term
need agent to treat migraines by alphaR-mediated constriction of vessels, that is, adrenalin reversal.  Use:
Definition

ergot derviatives

ergotamine or ergonovine

 

a-1 partial agonist (also serotonergic)

Term
PDE inhibitors that produce SYMP-like effects in body "sympathomimetic-like"
Definition

caffeine

theophylline

Term
another sympathomimetic-like drug that inhibits PDE to produce SYMP-like action; specifically targets PDE expressed in the penis to cause relaxation of smooth muscle in penis and allow prolonged blood flow
Definition
sildenafil (VIAGRA)
Term
need a short-acting reduction in sympathetic tone for surgery, but still get cardiac stimulation.  Use:
Definition

phentolamine

 

non-selective alphaR competitive antagonist

cardiac stimulation due to alpha2 inhibition in heart -->persistent NE

Term
need a long-acting way to block sympathetic tone, but it causes postural hypotension. use:
Definition
phenoxybenzamine
Term
need a 2nd line HTN drug b/c target is not reached yet in your patient, but want something that does not increase HR or CO.  But watch out for "first dose phenomenon".  use
Definition

prazosin

prototype alpha1 selective antagonist

Term
need something to treat benign prostatic hypertrophy that is causing lower UT symptoms (frequency, urgency, burning). Beware -- it can cause reverese ejaculation or priapism! use:
Definition

terazosin

 

alpha1-selective antagonist

a1Rs predominate in smooth muscle of bladder, urtehra and prostate

Term
an alpha adrenergic antagonist that actually increases NE release!
Definition
yohimbine
Term
this class of drug is governed by the concept of reducing oxygen demand of the heart to prevent heart diseases and ischemia
Definition
beta blockers
Term
need a beta blocker that will cross the BBB or placenta and get excreted by the liver; non-selective
Definition
propanolol
Term
need an agent that will lower IOP by decreasing sympathetic effects of beta receptors, non-selective.  Use:
Definition
timolol
Term
a beta-1 selective blocker that is also moderately lipid soluble
Definition
metoprolol
Term
a non-selective beta blocker that has the additional vasodilator action of blocking a1R.  need this in HTN emergencies b/c great for lowering BP short term.  Use:
Definition
labetalol
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