Mech: activates antithrombin III → decr. IIa (thrombin) & Xa

Tox: hep-induced thrombocytopenia (hep binds plts → autoAb's destroy & overactivate remaining plts → decr. plts, but hypercoag); osteoporosis

Use: immediate coag; can use during preg (doesn't cross placenta)

Antidote: protamine sulfate [(+)-charged, binds (-)-charged hep]Note: must follow PTT (intrinsic); short t1/2; admin IV/SQ

Low-molecular-wt heparin

Mech: activate antithrombin III → act more on Xa than IIa (thrombin)

Use: immediate anticoag; can use during preg

Notes: better bioavil & longer t1/2 than hep; can be admin SQ w/o lab monitoring; not easily reversible

Hirudin derivative

Mech: directly inhib thrombin

Use: anticoag in pts w/ HIT

Hirudin derivative

Mech: directly inhib thrombin

Use: anticoag in pts w/ HIT

(AKA: Coumadin)

Mech: blocks γ-carbox of vit K-dep factors (II, VII, IX, X; C, S)

Use: chronic anticoag; not in preg (crosses placenta)

Tox: bleeding, teratogenic, skin/tissue necrosis

Antidote: IV vit K + fresh frozen plasma

Note: metab by P-450; monitor PT/INR (extrinsinc pathway); admin PO

Thrombolytic

Mech: forms anistreplase with proactivator → converts plasminogen=>plasmin → plasmin degrades fibrin & fibrinogen

Use: early MI/stroke

Tox: bleeding

Antidote: aminocaproic acid (inhibs plasminogen=>plasmin)

Contra: intracranial bleed, recent surg, bleeding d/o, severe HTN

Note: incr. PT & PTT; no effect on plts

Thrombolytic

Mech: converts plasminogen=>plasmin → plasmin degrades fibrin & fibrinogen

Use: early MI/strokeTox: bleeding

Antidote: aminocaproic acid (inhibs plasminogen=>plasmin)

Contra: intracranial bleed, recent surg, bleeding d/o, severe HTN

Note: incr. PT & PTT; no effect on plts

Alteplase

(tPA)

Thrombolytic; (AKA: tPA)

Mech: converts plasminogen=>plasmin → plasmin degrades fibrin & fibrinogen

Use: early MI/stroke

Tox: bleeding

Antidote: aminocaproic acid (inhibs plasminogen=>plasmin)

Contra: intracranial bleed, recent surg, bleeding d/o, severe HTN

Note: incr. PT & PTT; no effect on plts

Mech: irrev. acetylates & covalently binds COX-1 & 2 → prevents TXA2 & PG synth

Use: low dose - decr. plt aggr; intermed (300-2400 mg/d) - antipyretic & analgesic; high - anti-inflam

Tox: ulcer, bleeding, hypervent, Reye's synd (in kids w/ viral infxn), tinnitus (CN8), ARF w/ chronic use; depresses uric acid clearance (unless high dose)

Note: prolongs bleeding time; no effect on PT or PTT

Plt aggregation inhibitor

Mech: irrev. blocks ADP Rs on plts → inhibs GP IIb/IIIa expression

Note: Used on mechanical heart valves

Plt aggregation inhibitor

Mech: irrev. blocks ADP Rs on plts → inhibs GP IIb/IIIa expression

Tox: neutropenia

Plt aggregation inhibitor

Mech: MAb vs. GP IIb/IIIaTox: bleeding, thrombocytopenia

Plt aggregation inhibitor

Mech: 1) inhibs plt PDE → prevents cAMP breakdown → prevents granule release; 2) direct vasodilator

Use: tx intermittent claudication (periph a. dz)

Antineoplastic antimetabolite (S-phase)

Mech: folic acid analog → inhibs DHF reductase → decr. dTMP → decr. DNA synth

Use: CA, abortion, ectopic preg, RA, psoriasis

Tox: myelosuppression; liver fatty chg.

Antidote: leucovorin (folinic acid) 

Antineoplastic antimetabolite (S-phase)

Mech: pyrimidine analog → converted to 5F-dUMP → covalent complex w/ folic acid → inhibs thymidylate synthase → decr. dTMP → decr. DNA synth

Use: Cancer

Tox: myelosuppression; photosens

Antidote: thymidine (not leucovorin)

6-mercaptopurine

(6-MP)

Antineoplastic antimetabolite (S)

Mech: activated by HGPRTase → blocks de novo purine synth

Tox: marrow, GI, liver

Interact: incr. tox w/ allopurinol (metab by XO) 

Antineoplastic antimetabolite (S) (AKA: ara-C)

Mech: inhibs DNApol

Tox: leukopenia, thrombocytopenia, megaloblastic anemia

Alkylating agent (non)

Mech: activated in liver → covalently x-link DNA at guanine N-7

Use: CA, immunosuppressant

Tox: myelosuppression, hemorrhagic cystitis (prevent w/ mesna)

Alkylating agent (non)

Mech: activated in liver → covalently x-link DNA at guanine N-7

Use: CA, immunosuppressant

Tox: myelosuppression, hemorrhagic cystitis (prevent w/ mesna)

Alkylating agent (non) - Nitrosourea (others: lomustine, semustine, streptozocin)

Mech: req activation → alkylate DNA

Use: brain tumors (can cross BBB)

Tox: dizzy, ataxia

Platinum coord. complex (non)

Mech: x-link DNA via formation of ROS

Use: testic, bladder, ovary, lung CA

Tox: nephrotox (prevent w/ amifostine, a free radical scavenger), acoustic n. dmg

Platinum coord. complex (non)

Mech: x-link DNA via formation of ROS

Use: testic, bladder, ovary, lung CA

Tox: nephrotox (prevent w/ amifostine, a free radical scavenger), acoustic n. dmg

Alkylating agent (G2)

Use: CML, ablating marrow for hemato stem cell trampl

Tox: pulm fibrosis, hyperpigm

Anti-tumor AB (non) (AKA: adriamycin)

Mech: generates free rad.s → noncovalently intercalates in DNA

Tox: cardiotox (CHF), myelosuppression, alopecia, toxic extravasation

Anti-tumor AB (non)

Mech: generates free rad.s → noncovalently intercalates in DNA

Tox: cardiotox (CHF), myelosuppression, alopecia, toxic extravasation

Anti-tumor AB (non) (AKA: actinomycin D)

Mech: Intercalating agent

Use: Wilm's tumor, Ewing's sarcoma, rhabdomyosarcoma; used in kids

Tox: myelosuppression

Anti-tumor AB (non)

Mech: forms free rad.s → break DNA

Tox: Pulm fibrosis, skin chg. (discolor), only minimal myelosuppression

Note: Lance Armstrong refused w/ testicular CA

Antineoplastic (S)

Mech: inhibs ribonucleotide reductase → decr. DNA synth

Use: CA, sickle cell dz (incr. HbF)

Tox: marrow suppr, GI

Topo inhibitor (S/G2)

Mech: inhibs topo II & incr. DNA degr

Tox: myelosuppr, alopecia

Corticosteroid

Mech: triggers apop (even in non-dividing)

Tox: iatrogenic Cushing's; immunosuppr; cataracts; acne; osteoporosis; HTN; ulcers; hyperglyc; psychosis

SERM - partial estr agonist

Mech: antag in breast, ag in bone

Tox: incr. risk endometrial CA; hot flashes

SERM - partial estr agonist

Mech: antag in breast, ag in bone

Tox: no incr. risk endometrial CA (endometrial antag)

(AKA: Herceptin)

Mech: MAb vs. HER-2 (erb-B2)

Use: metastatic breast CA over-expressing HER-2

Tox: cardiotoxic

(AKA: Gleevec)

Mech: inhibs bcr-abl Tyr kinase (t[9;22])

Use: CML

Tox: fluid retention

Alkaloid (M)

Mech: bind tubulin → block MT polym → prevent formation of mitotic spindle

Tox: neurotoxic (blocks MT formation in axons → areflexia, periph neuritis); paralytic ileus

Alkaloid (M)

Mech: bind tubulin → block MT polym → prevent formation of mitotic spindle

Tox: blasts" bone marrow"

Mitotic spindle poison (M)

Mech: bind tubulin → hyperstabilize to prevent depol.

Use: ovarian & breast CA

Tox: myelosuppr, hypersens