Drug Chart Pharm 3

7/27/2019 Drug Chart Pharm 3

1/20

Mechanism of Action Use Adverse Effects

Acyclovir Competitive inhibitor of nucleic

acid polymerases

(when inserted instead of base

missing hydroxyl group so no

phosphodiester bond suicidesubstrate, chain terminator)

HSV, VSV, EBV Generally well tolerated but

high IV dosing can cause

nephrotoxicity and

neurotoxicity

Drug resistance acan dveleop

with mutation in viral TK or

viral DNA pol

Can have as much as 50% in

CSF

Can interact with AZT(severe

lethargy) and nephrotoxic

drugsOseltamivir

Selective Neuraminidase

inhibitor; sialic acid analogues,

inhibit viral neuraminidase,

which cleaves sialic acid residues

to facilitate release from host cell

(stop viral release from cell)

Influenza A and B, treat within

48 hrs of onset, reduces time of

illness

transient mild moderate GI

distress, minimized with food

eliminated primarily

unchanged in the kidneys so

decrease dose in kids and

those with renal impairment

Zidovudine (AZT) Nucleoside/Nucleotide ReverseTranscriptase Inhibitors (NRTI)

Fully phosphorylated forms (i)

compete for RT, and (ii) function

as chain terminators block

viral replication

suppression of HIV infection;elevate CD4 counts, AZT use

during pregnancy reduces HIV

transmission to fetus


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Indinavir (IDV) inhibition of HIV protease, which

essential for the production of

mature, mediates post-

translational processing of viralgene products, cleaves itself then

other products

HIV, combination therapy - metabolized primarily via

cytochrome CYP3A4, other

drugs acted on CYP3A4 may

accumulate to dangerouslevels other drugs inducing

CYP3A4 may increase

metabolism

- resistance develops rapidly,

buffalo hump, due to fat

redistribution

also hyperglycemia,

nephrolithiasis

- absorption of this drug

impaired by high fat meal

Penicillin G lactam ring fused to five

membered thiazolidine ring and

R group; lactams irreversibly

inhibit transpeptidases and

decrease cross-linkage of glycan

strands compromising the cell

wall

less susceptible to lactamase

Bactericidal at therapeutic

concentrations

Generally well tolerated but

10% have allergy to whole

class

GI problems: nausea,

diarrhea vomiting

penicillins work best against

actively growing bacteria,

thus bacteriostatic antibiotics

(chloramphenicol,

macrolides, tetracyclines)

interfere with their activity

low pH, dextrose solns,

aminoglycosides solns:


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inactivate lactam

probenecid (gout) blocks

renal excretion, active lactam in blood longer

Amoxicillin Inhibit cell wall synthesis Superinfection with

Clsotridium difficile;

alteration of normal flora

allows this bacteria to grow;

produces toxin causing

diarrhea

Amoxicilin/Clavulanic

Acid (Augmentin)

Amoxicillin Inhibit cell wall

synthesis and clavulanic acid is a

lactamase inhibitor

broader spectrum activity GI: diarrhea, nausea, vomiting

most common with this

combination drugCeftriaxone Cephalosporin; inihibit cell wall

synthesis

3rd generation, broader

spectrum activity

Prolonged use causes biliary

sludging (pain, nausea,

vomiting) in up to 43%

Ciprofloxacin are bactericidal and target

topoisomerases which increased

the supercoiling of DNA which

impacts DNA replication, repair

and transcription

tolerated by humans well

because the drug has a greater

affinity for bacterial

topoisomerases and bacteria are

actively growing (replicating and

repairing DNA more)

metals chelate quinolones,

block adsorption; many

antacids, some dietary

supplements; take quinolones

2 hrs prior or 2-6 hrs after

digesting metals

Avoid in children,

pregnant/nursing women

(damage growing cartilage)

avoid in patients taking

drugs prolonging QT


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interval, arrhythmias,

fainting

TMP/SMX antifolate Recurrent UTIs, opportunistic

infections in AIDS

antifolate activity in humans,

may be offset withsupplement folic acid;

nephrotoxicity avoid in

renal impaired

Azithromycin Protein synthesis inhibitors;

bacteriostatic

treat infections caused by

Gram-positive bacteria; also

works well against several

Gram-negatives

Contraindication: hepatic

impairment

Antacids lower the serum

level of Azithromycin

GI: cramps, diarrhea, nausea,

vomiting

Erythromycin Protein synthesis inhibitors;

bacteriostatic

treat infections caused by

Gram-positive bacteria

Contraindication: hepatic

impairment

Drug Interactions:

Erythromycin inhibits the

cytochrome P450 System

(CYP3A4); interactions

common with other drugs

metabolized by CYP3A4

stimulates GI motility; GI

intolerance may force switch

of drug


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Cardiotoxicity: arrhythmia,

do not administer wih drugs

that prolong QT interval

Doxycycline Protein synthesis inhibitors;bacteriostatic

Caution: children under 8years; pregnant lactating

(category D); patients with

liver impairment

GI distress in some cases

GERD, Photosensitivity

Skeletal: avoid use in children

as drug binds bones and teeth

Rifampin inhibits DNA-dependent RNA

polymerase, blocks txn binds to

bacterial form with greater

affinity than eukaryotic

counterpart

combo treatments (TB,

leprosy); Also inhibits many G+

and G- bacteria; Prophylaxis of

meningococcal and H.

influenzae meningitis

generally well-tolerated,

minor hepatotoxicity, usually

in patients with prior liver

problems

induces P450 enzymes;

increases metabolism of

drugs processed by P450

enzymes

Isoniazid inhibits mycolic acid (FA)

synthesis, a unique component

of mycobacterial cell walls

Used alone for prophylaxis, in

combo to treat TB

Bactericidal for growing forms

Bacteriostatic for resting forms

hepatotoxicity, peripheral

neuritis can offset with

pyridoxine (vit B6), rash,

convulsions in patients prone

to seizure


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Amphotericin B binds ergosterol and forms pores

on the membrane

most systemic fungal infections,

some protozoa

amphoterrible,

fever and chill (shake and

bake), hypotension,

nausea,nephrotoxicity(80%)

caution with other

nephrotoxic drugs,

arrhythmias

caution in use: renal

impairment

Terbinafine interfere with ergosterolsynthesis (inhibit SQUALENE

EPOXIDASE) accumulate toxic

squalene compromise integrity

of membrane

dermatophytes nail fungus(onychomycosis), jock itch (T.

cruris), athletes foot (T. pedis)

generally well tolerated,avoid if pregnant/nursing or

if liver/kidneys impaired

Itraconazole interfere with ergosterol

synthesis, inhibits Lanosterol -

14- Demetylase, a cytochrome

P450 enzyme

Broad spectrum avoid azoles in pregnancy

Griseofulvin binds microtubules- mitosis

inhibitor (causes multinucleated

cells)

restricted to dermatophyes

(skin, hair and nail infections),

alternate treatment for

onychomycosis (nail),

ringworm caused by

Microsporum, Epidermophyton

Generally well tolerated;

headaches other CNS effects,

photosensitivity and rash


7/20


8/20

Sulfadiazine +

Pyrimethamine

DHPS & DHFR inhibitor, resp.;

blocks production of THFA

Toxoplasma, antimalarial,

antibacterial

allergies to sulfa,

pyrimethamine toxicity (bone

marrow suppression), does

not alleviate encysted formMebendazole Inhibits microtubule

polymerization/mitotic spindle

poison; bind worm -tubulin

with higher affinity than

mammalian orthologue

nematodes/roundworms Generally well tolerated

Ivermectin kills larvae in host not effective

against adult worm; induces

paralysis via glutamate gated Cl-

channels found only ininvertebrates

broad spectrum antiparasitic;

nematode, esp. for filariae

causing onchocerciasis (river

blindness)

Can effect mammalian GABA

receptor so contraindicate

when Blood Brain Barrier

is impaired

Praziquantel causes spastic paralysis and

tegument damage

flatworms and cestodes generally well tolerated, GI

distress, CNS effects

Contraindications:ocular

cysticercosis (tapeworm

larvae in eye) as host

response to dead worm

damages eye;

ophthalmologic surgery is

recommended instead

inducers of CYP reduce

bioavailability of drug

Insulin Type 1 DM; IDDM Hypoglycemia;


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impaired neurologic function.

inability to concentrate.

slurred speech, lack of

coordination, staggering

symptoms are often

mistaken as alcohol

intoxication

Glipizide increasing endogenous insulin

secretion;ATP binds to KIR and

blocks the channel

ADP binds to SUR and

activates the channelSUR enhances sensitivity of

KIR to ATP and interacts with

sulfonylureas and

meglitinides

Type 2, NIDDM

Oxidized to inactive metabolites

Half-life - 2 to 4 hours

Potency - High (2.5 to 40

mg/day)

hypoglycemia

Glyburide increasing endogenous insulin

secretion ;ATP binds to KIR

and blocks the channel

ADP binds to SUR and

activates the channel

SUR enhances sensitivity of

KIR to ATP and interacts with

sulfonylureas and

meglitinides

Type 2, NIDDM

Oxidized to weakly active

metabolites

Half-life - 6 hours

Duration of action - 24 hours

Potency - High (1.25 to 20

mg/day)

hypoglycemia

Repaglinide Decrease ATP sensitive K+ Tyoe 2, NIDDM Effect is rapid and brief so


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channel conductance

Act similarly too sulfonylureas

but bind to distinctly different

region of SUR1

reduced risk of long-lasting

hypoglycemia

Metformin Insulin sensitizers;

antihyperglycemics; Correct

elevated hepatic glucose

output

Inhibit hepatic gluconeogenesis

Inhibit glucose-6-phosphatase

activity inhibit glycogenolysis activity of insulin receptors

insulin resistance

Appropriate for obese type 2

diabetics

Doesnt produce lactic

acidosis or hypoglycemia;

Secondarily Reduced

triglycerides, total

cholesterol, LDL

Increased HDL

Weight loss, some reduction

of blood pressurePioglitazone are agonists of -(PPAR)

activation of PPAR alters therate of expression of a number of

genes encoding proteins

involved in regulating lipid and

glucose metabolism, ultimately

increasing sensitivity to

insulin at the target tissues

DM Reduce hepatic glucose

output

Does not increase insulin

secretion

Does not induce weight gain

Acarbose competitive and reversible

inhibitors of a-glucosidase in

the small intestine

Delay carbohydrate digestion

and absorption

Smaller rise in postprandial

glucose

For mild to moderate fasting

hyperglycemia with significant

postprandial hyperglycemia

Gastrointestinal disturbances

Flatulence

Nausea

Diarrhea

Contraindicated for

inflammatory and

obstructive bowel

disease, colonic ulcers


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Diazoxide opens the KATP channel and

inhibits insulin release

Oral agent for hypoglycemia

of various causes, including

insulinomas

Levothyroxine Synthetic T4 hormone Hypothyroidism Rare but excessive dose

produce symptoms of

hyperthyroidism

Propylthiouracil compete with thyroglobulin for

oxidized iodide in the process of

organification and coupling

inhibits T4/T3 conversion

Hyperthyroidism

Propylthiouracil inhibits both

thyroid peroxidase and T4/T3

conversion

Methimazole compete with thyroglobulin for

oxidized iodide in the process oforganification and coupling

Hyperthyroidism

methimazole inhibits only

thyroid peroxidase; more

potent than propylthiouracil

Radioactive iodide results in selective destruction of

thyroid gland

hypothyroidism

Stable Iodide high levels of iodide inhibit

thyroid hormone synthesis and

release (Wolff-Chaikoff effect)Hyperthyroidism

used to block thyroid function

in radiation emergencies

hypothyroidism

Propanolol inhibit peripheral T4/T3

conversion by 5-deiodinase

Hyperthyroidism

Inihibit peripheral thyroid

metabolism

Alendronate inhibit mevalonate pathway in Pagets disease and not to be used in the presence


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osteoclasts, posttranslational

modification

slow or block bone resorption,thus, help to lower serum

calcium levels

postmenopausal osteoporosis

in women

of hypocalcemia, during

pregnancy or lactation, or

with a history of any allergy

to bisphosphonates

should not be given to anyone

who is unable to remain

upright for 30 min after

taking the drug, then to have

a meal serious esophageal

erosion can occur!

Calcitonin binds directly to receptors on

osteoclasts and inhibits bone

resorption;

Antihypercalcemic salmon calcitonin should not

be used with known allergies

to salmon or fish products

caution should be used in

patients with renal

dysfunction could be

exacerbated

flushing of the face and

hands, skin rash, nausea and

vomiting,

urinary frequency, localinflammation at the site of

injection

Calcitrol Increases absorption of dietary

calcium in small intestines

Vit D compound

reatment of

hypoparathyroidism and in

patients undergoing chronic

renal dialysis

should not be used in the

presence of any known

allergy to vitamin D,

hypercalcemia, vitamin D


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mineral resorption in bone, and

re-absorption of calcium and

phosphate from renal tubules

inhibit PTH synthesis and

release

with PTH and calcitonin regulate

calcium homeostasis

toxicity

metallic taste, nausea,

vomiting, dry mouth,constipation, and anorexia

CNS effects: weakness,

headache, somnolence,

irritability

Calcium gluconate a therapy for hypocalcemic

states associated with disorders

such as vitamin D-dependentrickets and

hypoparathyroidism

less venous irritation than

calcium chloride

Parathyroid Hormone increase in bone formation

occurs because PTH acutely

promotes osteoblast

development and stimulates

osteoblast activity

stimulates production of active

vitamin D in the kidney

once-daily subcutaneous

administration of PTH favors

bone anabolism

cannot be taken orally, only

subcutaneously or IV


14/20

Methotrexate Inhibition of dihydrofolate

reductase (DHFR) which leads to

depletion of cofactors required

for synthesis of thymidylate andpurines

ALL in children,

choriocarcinoma, combo

therapy for breast carcinomas,

head and neck, ovary andbladder high dose used for

adjuvant therapy

Also for psoriasis, rheumatoid

arthritis, immunosuppressive

agent

With standard dose

myelosuppression, stomatitis,

enteritis

High dose have conjunctivitis,

renal failure neurotoxicity

and rarely hepatic failure

6-Metacaptopurine Function as analog of natural

purine and inhibit de novo

purine synthesis and become

incorporated into nucleic acids

Myelosuppression, gi and

hepatic toxicity

5-Fluorouracil Inhibition of thymidylate

synthase, reduced production of

TTP increase incorporation of

dUTP into DNA

Potent radiosensitizer

Intense dense and combo

with leucovorin associated

with significant gi toxicity,

myelosuppression

Skin pigmentation and rashes

are common

Rarely cerebellar toxicity


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Gemcitabine Inhibition of ribonucleotide

reductase; inhibit incorporation

of dCTP into DNA by DNA pol

IV administration only Same toxicities as the class

and elevation in liver

transaminases

Potent radiosensitizer, not to

be used with radiotherapy

Vinblastine Bind to tubulin at site that

overlaps with GTP binding

domain and prevents extension

of MTs; chromsomes dont

segregate during mitosis

Lymphomas and second line

therapy for various solid

tumors

Neutropenia; gi side effects

Paclitaxel Bind to beta tubulin at site

distinct from vincas or colchine;

promote polymerization and

prevent depolymerization

arresting cell in mitosis

Treatment of many solid

tumors breats, ovarian and

lung

Peripheral neuropathy,

myalgias, myelosupression

Acute hypersensitivity rxns

occur possibly die to vector

Docetaxel Same as above, arrests cell in

mitosis

Improves survival in men with

metastatic prostate cancer by

2.4 months



Cabazitaxel Same as above, arrests cell in

mitosis

Improves survival in men with

metastatic prostate cancer by

4.3 months




16/20

Colchine Bind MTs at interface btw alpha

and beta tubulins, and

destabilize

First used as anti-

inflammatory/immune

Used in association withallopurinol for gout

Immune deficiency, diarrhea

Cyclophosphamide Alkalating agent; alkylates DNA

twice inducing crosslinks in the

DNA

Metabolite acrolein, can

cause severe cystitis, fancoli

like syndrome in kidneys

CNS: confusion, drowsiness,

hallucinations

Temozolomide Standard of care for

glioblastomas; lipid soluble candiffuse across BBB

Myelosuppression

TMZ+ O6- Benzyl

Gaunadine

Binds DNA repair and

potentiates effects of other

chemotherapy agenst that

damage DNA

Doxorubicin Intercalate into GC rich regions

of DNA, depress DNA,RNA and

protein synthesis

May metabolize and form free

radicals

Activate apoptosis signaling

pathway

Myelosuppression, alopecia,

GI disturbances, cardiac

toxicity is marked


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Cisplatin Functional groups replaced by

water which is replaced by DNA

base usually G and crosslinking

occurs

Nephrotoxicity common,

highly emetogenic, marked

peripheral neuropathy,

anemiaCarboplatin Functional groups replaced by

water which is replaced by DNA

base usually G and crosslinking

occurs

Nephrotoxicity only in high

doses, mildly emetogenic,

rarely have peripheral

neuropathy,

myelosuppression

Etoposide Cause DNA strand breaks by

trapping and stabilizing top II

Tamoxifen Blocks estrogen receptor Breast cancer

Degaralix Blocks GnRH Breast cancer

Imatinib Philadelphia chromosome CML

Trastuzumab Interferes withHER2/neureceptor

Breast cancer
http://en.wikipedia.org/wiki/HER2/neuhttp://en.wikipedia.org/wiki/HER2/neuhttp://en.wikipedia.org/wiki/Receptor_(biochemistry)http://en.wikipedia.org/wiki/Receptor_(biochemistry)http://en.wikipedia.org/wiki/HER2/neu


18/20

Tocilizumab IL-6 receptor antagonist

(cytokineinvolved in thedevelopment of immunological

and inflammatory reactions)

Bevacizumab antibody that blocks vascular

endothelial growth factor A

(VEGF-A) which prevents the

establishment of blood supply

and metastatic spread.

RCC, lung cancer, colon cancer

to slow growth and inhibit

spread


19/20

Clomiphene Anti-estrogen , blocks estrogen

inhibition of FSH and LHrelease

Used to treat ovarian failure Possibility for

overstimulation multiplepregnancies

Menotropins/ Urofillitropin Produces follicular stimulation

hCG Mimics LH, After priming with

menotropins for 14 days

give hCG to induce follicle

ovulation

Danazol Synthetic androgen used to

inhibit the output of FSH/LH,

removing hormonal

stimulation

Treatment for

endometriosis

Any sex steroid caninhibit FSH/LH in either

sex

Facial hair, lose hair, and

slight virilization

GnRH Stimuates the release of

LH/FSH

Must administer in a

pulsatile pattern

estradiol Endogenous First pass effect so not

effective orally

Estrone Major endogenous estrogen in

humans

Conjugated estrogens Equillan

Premarin

Purified mixtures of

conjugated steroids with

estrogenic properties

Ethinyl estradiol Slower; orally available

Mestranol Orally effective prodrug;

quickly demethylated to

ethinyl estradiol


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Progesterone Progesterone analogs Progestational activity

medroxyprogesterone Progesterone analogs Progestational activity

Slow release form f injectedprogesterone, once injected

slowly ansorbed into

circulation, once n

circulation they are rapidly

transformed and cleared

aaw

Norethindrone Progestational and androgenic

activity

Drosperinone Anti-androgemic activity and

anti mineralcorticoid activity,

available in combo type oral

contraceptives

Norgesetrel, levonogestrel Progestational and androgenic

activity

Mifepristone RU- 486 abortion pill

Drug Chart Pharm 3

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