drug list Flashcards
what’s the first antisense drug to be approved by FDA?
vitravene
what’s used in the treatment of CMV retinitis?
vitravene
what is only effective in about 20% of patients that overexposes HER2 receptor?
Herceptin
Herceptin aka
trastuzamab
what is a metastatic breast cancer treatment ?
Herceptin
what drug may lead to cardio toxicity and ADRs?
Herceptin
following patient testing what’s one of the first drugs to be prescribed for patients with breast cancer?
Herceptin
what are the two MOA of Herceptin?
1 prevent HER2 receptor from releasing growth signals
2 it will tell your immune cells to target cells with HER@ receptor
what happens in the absence of Herceptin?
HER2 cancer cells release excess growth signals for proliferation
what drug is metabolized by isoenzyme CYP2D6?
debrisoquine
what kind of drug is debrisoquine?
antihypertensive
what alter metabolism of debrisoquine?
SNPs in the isoenzyme
what drugs follow zero order kinetics?
ethanol and aspirin
ethanol is excreted in …
sweat
what’s penicillin?
an acidic antibiotic
how are penicillin and aspirin excreted?
via proximal tubular secretion (renal excretion)
what is used in the excretion of penicillin and aspirin?
anion transport system
what may prolong effects of penicillin?
competition for secretion with probenecid
what is aspirin?
acidic salicylate
what is given to prevent gout?
aspirin is given to compete with uric acid during distal tubular active reabsorption
what drugs are alkylating agents ?
cyclophosphamide and thio-TEPA
cyclophosphamide and thio-TEPA MOA
creates highly reactive carbonium ion which alkylates guanine at N-7 position
what prodrug is acts on S/G2 phase and G2/M phase?
cyclophosphamide
what activates cyclophosphamide?
CYTP450
what drug is used for treatment of chronic lymphatic leukemia?
cyclophosphamide
what drug is used for treatment of breast and ovarian cancer?
cyclophosphamide
what drug is used in the management of rheumatic disorders and autoimmune nephritis?
cyclophosphamide
what are the adverse effects associated with cyclophosphamide and thio-TEPA ?
myelosuppression
nausea and vomitting
teratogenesis
gonadal atrophy
what drugs carry risk of leukomegenesis and resistance?
cyclophosphamide and thio-TEPA
what drug is aka as ethyleneammonium?
thio-TEPA
how is thio-TEPA activated?
its converted into its active metabolite try ethylene phosphor amide by liver MFO
what’s used in the treatment of bladder cancer?
thio-TEPA
what are antimetabolites used to treat cancer?
methotrexate (MTX) and 5-fluorouracil (5-FU)
what drug is a folic acid antagonist?
methotrexate (MTX)
what does methotrexate (MTX) do?
irreversibly inhibits DHFR which is needed for thymidine and purine synthesis
what drug is a prymidine antagonist?
5-fluorouracil (5-FU)
what drug is a thymine analogue that has a fluorine group instead of a methyl group?
5-fluorouracil (5-FU)
what does 5-fluorouracil (5-FU) do?
its active metabolite 5-dUMP inhibits DNA synthesis and 5-dUTP when incorporated into RNA prevents its function
what’s used in treatment of solid tumors?
5-fluorouracil (5-FU)
what’s used in treatment of breast tumors?
5-fluorouracil (5-FU)
what’s used in collateral tumors and gastric tumors?
5-fluorouracil (5-FU)
what’s used in the treatment of squamous cell tumors of the head and neck?
5-fluorouracil (5-FU)
what are adverse effects of methotrexate (MTX) and 5-fluorouracil (5-FU)?
myelosuppresion severe leukopenia bone marrow aplasia hepatotoxicity thrombocytopenia gi disturbances crystal urea
what drugs are G1/S and S/G2 specific?
methotrexate (MTX) and 5-fluorouracil (5-FU)
what drugs intercalate btwn bps –> topoismoerase ii inhibited and free radicals fare formed –> inhibition of. dna synthesis and cause strand incision?
Doxorubicin and Actinomycin D
what drug is an anthracycline?
Doxorubicin
how does Doxorubicin work?
It gets reduced by CYTP450 reductase into a reduced metabolite and a superoxide ion hydrogen peroxide, which breaks the strands in DNA
what drugs may lead to severe cardiac toxicity and serious pulmonary and mucocutaneous reactions because of their free radical formation?
Doxorubicin and Actinomycin D
what are the adverse effects of Doxorubicin and Actinomycin D?
Cardiac toxicity
Severe pulmonary and mucocutaneous reactions
Bone marrow depression
Severe and prolonged Myelosuppression
Total alopecia
It is a cell cycle specific
drug: G1/S and G2/M
Actinomycin D
It’s used to treat
gestational and pediatric
tumors (Ewing Sarcoma
and Wilms Tumor)
Actinomycin D
It intercalates DNA and
inhibits DNA and mRNA
synthesis.
Actinomycin D
what drug causes excess hypotension in poor metabolizers ?
Debrisoquine
what drug is an antidepressant?
paroxetine
what affects response of paroxetine?
Its response is affected by
SNPs in the Serotonin 2A
receptor.
whats the purpose of paroxetine?
It is a serotonin reuptake
inhibitor.
what was found in patients taking paroxetine?
They found that depressed patients with the C/C genotype for the serotonin 2A receptor were more likely to discontinue the use of Paroxetine then the T/C and T/T genotype.
name an endogenous adrenergic
agonist
nora
what are the Direct-acting adrenergic
agonist?
Nora phenylephrine clonidine isoprenaline dobutamine salbutamol
what receptors does NA act on?
alpha 1 and alpha 2
NA is a catecholamine what does that mean?
can’t be ingested orally bc it will be digested by MAO and COMT before it reaches systemic circulation ( short DOA)
cannot pass the BBB so minimal effect on CNS
what blocks release of NA from presynaptic neuron?
guanthedine
what direct acting adrenergic agonists are sympathomimetic?
phenylephrine
clonidine
dobutamine
salbutamol
true or false phenylephrine can be given orally.
true
what drug is a selective alpha 1 adrenergic agonist?
phenylephrine
what drug causes vasoconstriction?
phenylephrine
what drug is used as a nasal decongestant?
phenylephrine
why is phenylephrine used as a nasal decongestant?
acts on alpha 1 receptors on bvs of nasal mucosa to relieve congestion by inducing vasoconstriction
what is a selective alpha 2 adrenergic agonist ?
clonidine
what is used to treat hypertension by inhibiting sympathetic outflow leading to decreased blood pressure?
clonidine
what inhibits NA release ?
clonidine
what drugs are catecholamines ?
NA
isoprenaline
what drug is a nonselective beta agonist?
isoprenaline
what is the effect when isoprenaline acts on B1 receptors?
increase renin release and contractility and rate of heart
what is the effect when isoprenaline acts on B2 receptors?
bronchodilation and peripheral vasodilation
what drug is a selective b1 adrenergic agonist?
dobutamine
what drug increases cardiac output and contractility of heart?
dobutamine
whats useful in Tx of CHF by increasing cardiac output?
dobutamine
how does dobutamine indirectly increase heart rate?
increase release of renin from kidneys promoting release of angiotensin II which brings up heart rate
what drug is a selective B2 adrenergic agonist?
salbutamol
whats used in the treatment of asthma for its bronchodilator effect?
salbutamol
whats used in the treatment of premature labor because it relaxes the smooth muscles of the uterus?
salbutamol
what drug is a nonselective alpha adrenergic blocker?
phentolamine
whats used to treat hypertensive crisis cause by phaeochromocytoma?
phentolamine
phentolamine …… until tumor ( phaeochromocytoma) is removed.
release of catecholamines
whats a selective alpha 1 adrenergic antagonist ?
prazosin
whats used in treatment of primary hypertension?
prazosin
what is used to treat benign symptoms of prostatic hyperplasia?
prazosin
how does prazosin treat benign symptoms of prostatic hyperplasia?
prevents contraction of urinary smooth muscles and bladder neck allowing urine to pass easily and reducing lower UT symptoms
what drug is a nonselective beta antagonists?
propranolol
It is a selective B1
adrenergic agonist
Dobutamine
It increases the cardiac
output and contractility of
the heart.
Dobutamine
• It is useful in the
treatment of CHF by
increasing the CO.
Dobutamine
It also can increase the release of renin from the kidneys promoting the release of angiotensin II which brings up the heart rate.
Dobutamine
It is a selective B2
adrenergic agonist
Salbutamol
Used in the treatment of Asthma for its bronchodilator effect and in the treatment of premature labor (relaxes the smooth muscles of the uterus).
Salbutamol
Non -selective alpha - adrenergic blocker (Acts on both alpha 1 and alpha 2)
Phentolamine
It is used to treat hypertensive crises caused by phaeochromocytoma (which is a tumor of the adrenal glands that secretes excess catecholamines)
Phentolamine
__________ prevents
the release of
catecholamines until the
tumor is removed.
Phentolamine
Selective alpha 1
adrenergic antagonist
Prazosin
It is useful in the
treatment of primary
hypertension.
Prazosin
It is used to treat symptoms of benign prostatic hyperplasia. It prevents contractions of the urinary smooth muscles and bladder neck allowing the urine to pass easily and reducing lower UT symptoms.
Prazosin
Non -selective beta - adrenergic antagonist (blocks beta 1 and beta 2).
Propranolol
• It blocks the effects of
catecholamines on the
heart and blood vessels.
Propranolol
Is used to treat angina pectoris - chest pain caused by lack of O2 to the heart (because of increased blood flow). \_\_\_\_\_\_\_\_\_ decreases the CO and BP allowing time for the blood to pass through the heart.
Propranolol
Considered as a first line treatment for hypertension and can be used in combination with other blood pressure lowering drugs to maximize the affect.
Propranolol
It is also proven to have a protective affect in patients who have had a MI (prevents them from getting it a second time so its protective on the heart)
Propranolol
It is also used in the treatment of hyperthyroidism (which can cause tachycardia and anxiety)
Propranolol
It can also decrease the bp
by decreasing the CO and
renin release.
Propranolol
AE: Since it is non
-selective
it may cause
bronchospasm in patients
who have asthma.
Propranolol
AE: It may also lead to
cardiac depression and
signs of HF.
Propranolol
It is used in the treatment of hypertension and may be used in combo with other blood pressure lowering drugs.
Atenolol
used in the
treatment of angina
pectoris.
Atenolol
It is used to treat MI
protective effect
Atenolol
used to treat
hyperthyroidism
Atenolol
AE : cardiac depression and HF
Atenolol
• It also decreases bp by
decreasing the CO and
renin release.
Atenolol
It blocks the effect of
catecholamines on the
heart and blood vessels.
Atenolol
Indirect acting adrenergic agonists
cocaine tricyclic antidepressants amphetamine tyramine MAO inhibitors
direct acting adrenergic agonists
dopamine
epinephrine
isoproterenol
mixed action adrenergic agonists
ephedrine
It inhibits neuronal uptake
uptake 1
cocaine
tricyclic antidepressant
It increases the amount of NA in synaptic gap and thus promotes increased activation of adrenergic receptors (both
cocaine
tricyclic antidepressant
tricyclic antidepressant
Imiprimane
It blocks the release of NA
into synaptic space.
Guanethidine
Noradrenergic neuron
blocking drug
Guanethidine
Drugs that act on
noradrenergic nerve
terminals
Reserpine
It blocks the transport of
NA into synaptic vesicles,
thus depleting the stores.
Reserpine
It is not used clinically.
Reserpine
It does not bind to a receptor instead it displaces NA from the vesicles to cause NA release.
Amphetamine
MOA: it enters the nerve terminal via uptake 1 and enters the synaptic vesicle in exchange for NA. This causes NA to accumulate presynaptically and some of it will be broken down by MAO, while the rest of it will be released into the synaptic cleft to act on adrenergic receptors.
Amphetamine
It acts in a similar way to
amphetamine (ya3ny it
displaces NA from its
vesicle)
Tyramine
It can cause severe
hypertension in patients
who take MAO inhibitors.
Tyramine
It is naturally broken down
by MAO (you can see why
MAO inhibitors are a
problem)
Tyramine
A protein found in cheese
products
Tyramine
It is involved in the cheese
reaction.
Tyramine
Mixed acting adrenergic agonist (ya3ny it can increase the amount of NA released or it can bind to the receptors and activate them directly)
Ephedrine
Non-catecholamine
Ephedrine
It is the major
neurotransmitter of the
PSNS
Acetylcholine
It is an endogenous and direct acting
cholinergic agonist
Acetylcholine
It is involved in the PSNS and
acts on nicotinic or
muscarinic receptors.
Acetylcholine
Typically acts on skeletal
muscles in the somatic
efferent pathway
Acetylcholine
It is the major neurotransmitter in all presynaptic neurons of the PNS and is only active in the PSNS post-synaptically.
Acetylcholine
Heart: decreases CO
and rate of the heart
Blood vessels:
vasodilation and
decreased blood
pressure
Acetylcholine
GI: stimulates
salivary and
intestinal secretion
and gastric motility
Acetylcholine
Lungs: it induces
bronchiolar
secretion and
bronchoconstriction.
Acetylcholine
Genitourinary tract: it increases the detrusor urinae muscle tone for expulsion of urine.
Acetylcholine
Eye: muscle
contraction for near
vision and pupil
constriction (miosis)
Acetylcholine
It is broken down by
acetylcholinesterase
Acetylcholine
It activates all cholinergic
receptors (muscarinic and
nicotinic receptors)
Acetylcholine
It is not used therapeutically because of its multiplicity of action and its rapid degradation by acetylcholinesterase.
Acetylcholine
