Unit 4 Drugs in Random Order Flashcards

(112 cards)

1
Q

Bevacizumab

A

Tx: Cancer

Mech: blocks VEGF

Prevents Vascular epi. growth factor from binding to receptor

Tumor can only grow w/ blood supply-this blocks it

_Beave_rs are _veg_etarians

Beva-cizumab–VEGF

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2
Q

Dactinomycin

A

Tx: Cancer

Mech: Intercalates w/ DNA and interferes w/ mRNA synth

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4
Q

Tripelennamine

A

First gen H1 blocker

Tx: Sedative, local anesthetic effect

Pharmacokinetics: Slightly lipid soluble, not ionized→Gets into CNS

Toxicity:

  • High TI
    • But suicide attempts b/c readily available
  • Interactions w/ other CNS depressants
  • Anti-muscarinic effects
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4
Q

Fexofenadine

A

Second gen H1 blocker

Pharmacokinetics: Ionized in blood so fewer CNS effects

Don’t cause drowsiness

Not metab by P450

Toxicity:

  • High TI
    • But suicide attempts b/c readily available
  • Anti-muscarinic effects
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5
Q

Prednisone

A

Tx: Asthma

DOC for prophylaxis

Mech: Bind intracellular receptor→altered DNA transcription

Activate receptor

Increase lipocortin→inh. synth of phospholipase A2 (precursor of prost and leukotriene)

Route: Not inhaled

SE:

  • Infections (esp mouth)-thrush
  • Dysphonia (diff. speaking)
  • Systemic effects
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5
Q

Abatacept

A

Tx: RA

Immunosuppressant

Mech: binds to and inh. CD80, CD86 receptors

Affects T cell activation

ABatacept CD80+86 receptors

_A_batacept for _A_rthritis

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5
Q

Ibritumomab

A

Tx: Cancer

Mouse MAB

Severe infusion rxn

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6
Q

Sulindac

A

NSAID

Acetic acid derivative

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7
Q

Tamoxifen

A

Tx: Cancer

Mech: Blocks estrogen receptor

SE:

  • Cataracts
  • Retinal changes

Tammy is as big as an ox because her estrogen receptor is blocked. She’s obsessed w/ Ron Swanson and has CRazy eyes

Tamoxifen blocks estrogen receptor. Side effects associated w/ eyes: Cataracts and Retinal damage

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8
Q

Topotecan

and irinotecan

A

Tx: Cancer

Mech: inhibits topoisomerase 1

  • You know its a topoisomerase inhibitor but which one?*
  • Add the first letter of one vs two to the front. If it makes sense it’s correct*
  • ttopotecan vs otopotecan*
  • **O-topotecan so topoisomerase One***
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8
Q

Flutamide

and other “lutamides”

A

Tx: Cancer (prostate)

Mech: Blocks androgen receptor

Androgen receptor inside cell

Some tumors are hormone dependent

  • Careful:*
  • Flunomides-inh dihydroorate DH*
  • Flutamides-block androgen receptor*
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9
Q

Other NSAIDs

A

_Pyr_os _ne_ed _e_xcess _f_ire

_Pyr_oxicam _n_abumetone _e_todolac -_f_enac

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10
Q

6-mercaptopurine

A

Tx: Cancer

Mech: Converted in cell to an analog that inhibits several enzymes needed for purine synth

Prodrug–purine analog

  • Azathioprine=immunosuppressant prodrug. *
  • Gets converted into 6-mercaptopurine.*
  • Used for Chron’s, RA, and transplants*
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11
Q

Acetic acid derived NSAIDs

A

Double A (Aaron) slobbers into titties

Acetic Acid: Sulindac indomethacin tolmetin

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12
Q

Methotrexate

A

Tx: DOC early tx of RA

Used more as immunosuppressant than anti-cancer drug

DMARD-Disease modifying anti-rheumatic drug

Actually stops progression of RA rather than just treat symptoms

Mech:

  • Analog of Folic Acid
  • Inh. enzyme: Dihydrofolate reductase
  • PABA→Folic acidDihydrofolic acid⇒tetrahydrofolic acid
    • ⇒ indicate where DHFR works
  • Inh. mammalian cell division
    • Inh. lots of folic acid dependent processes, especially in cells w/ rapid turnover (at high doses):
      • GI
      • Fetal development
      • Blood cells
    • Immune cells more susceptible than above though
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13
Q

Clemastine

A

First gen H1 blocker

Tx: Motion sickness, sedative

Pharmacokinetics: Slightly lipid soluble, not ionized→Gets into CNS

Toxicity:

  • High TI
    • But suicide attempts b/c readily available
  • Interactions w/ other CNS depressants
  • Anti-muscarinic effects
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13
Q

Promethazine

A

First gen H1 blocker

Tx: Strong sedative, strong anti-emetic

Related to anti-psychotic drugs

Pharmacokinetics: Slightly lipid soluble, not ionized→Gets into CNS

Toxicity:

  • High TI
    • But suicide attempts b/c readily available
  • Interactions w/ other CNS depressants
  • Anti-muscarinic effects
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14
Q

Chlorpheniramine

A

First gen H1 blocker

Tx: Does not cause as much sedation

Pharmacokinetics: Slightly lipid soluble, not ionized→Gets into CNS

Toxicity:

  • High TI
    • But suicide attempts b/c readily available
  • Interactions w/ other CNS depressants
  • Anti-muscarinic effects
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15
Q

Cortisone

+

Hydrocortisone

A

Immunosuppressive potency=1

Relative minerallocorticod activity=1

Duration: 8-12hrs

Cortisone is a prodrug:

  • Must be metab by P450 (in liver)
  • Not effective topically
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16
Q

“-ergotamine”s

A

Ergotamine

Dihydroergotamine

Tx: Migrane

Mech: Partial 5HT receptor agonist

Can affect adrenergic and dopaminergic receptors

Useful in initial stages

SE:

  • Ergotism=excess of ergot alkaloids→St. Anthony’s Fire
    • Hallucinations (these are the source of LSD)
    • Uterine contractions-_preg. category X_
    • Severe vasospasm→gangrene (loss of O2 to periphery
  • ​Not as safe as triptans
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17
Q

Loratadine

A

Second gen H1 blocker

Pharmacokinetics: Ionized in blood so fewer CNS effects

Don’t cause drowsiness

Not metab by P450

Toxicity:

  • High TI
    • But suicide attempts b/c readily available
  • Anti-muscarinic effects
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18
Q

Mometasone

A

Tx: Asthma

DOC for prophylaxis

Mech: Bind intracellular receptor→altered DNA transcription

Activate receptor

Increase lipocortin→inh. synth of phospholipase A2 (precursor of prost and leukotriene)

Route: Inhalation

1st pass metabolism

SE:

  • Infections (esp mouth)-thrush
  • Dysphonia (diff. speaking)
  • Systemic effects
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18
Q

Golimumab

A

Tx: RA, Ulcerative colitis, psoriatic arthritis

Immunosuppressant

Mech: Binds TNF

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18
Q

Tolmetin

A

NSAID

Acetic acid derivative

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19
Atgam
**_ATG_**am Tx: **_A_**cute renal **_t_**ransplant injection Immunosuppressant **_A_**nti**_t_**hymocyte **_g_**lobulin (ATG)--Polyclonal antibodies Effects: Reduces circulating T cells(Wikipedia) ***_A_**ffects **_T_** cell activation* SE: * Polyclonal antibodies may lead to allergic rxn * From horse or rabbit
19
"-fenac"s
diclofenac bromfenac Nepafenac NSAID
20
Longer lasting relatively selective B2 agonists
Formoterol Arformoterol Salmeterol Indicaterol *"rols" w/o any "b"s​* Tx: Asthma Bronchodilator--**DOC** for short term relief Mech: B2 agonist--not completely selective Cause even more down regulation of B2 receptors Not as effective for rapid relief SE: * Tremors * Tachycardia * Heart palpitations * Indigo Salmon Asked For More* * Indigo Salmon Asked Fo mo'* ***_Ind_**icaterol **_Salmo_**eterol **_A_**r**_formo_**terol **_Formo_**terol*
21
Azathioprine
Tx: RA, Chron's, trans Prodrug Mech: * Converted to 6-mercaptopurine * Inh. synth of purines (guanosine required for DNA synth) * _Inh. several enzymes_ responsible for GMP synth * Non specific SE: * Bone marrow suppression→ * Megaloblastic anemia * Thrombocytopenia * Leukopenia *6-mercaptopurine is also an anti-cancer agent*
22
Diphenhydramine
First gen H1 blocker Tx: Sedative, motion sickness Pharmacokinetics: Slightly lipid soluble, not ionized→**Gets into CNS** Toxicity: * High TI * But suicide attempts b/c readily available * Interactions w/ other CNS depressants * Anti-muscarinic effects
23
Everolimus
Tx: Transplant, psoriasis Mech: Bind to FK binding protein _inh. kinase_ required for binding of IL-2 induced transcription factors to DNA→decreased cytokine production Often used in combination w/ glucocorticoids SE: * Some renal toxicity * Less than tacrolimus * Synergistic effect w/ used in comb w/ many immunosupp. * Some lung toxicity Metab by P450 ... * What else binds to FK protein? Tacrolimus* * Tacrolimus: Inh calcinuerin phosphatase* * Everolimus/Sirolimus: Inh kinase*
23
5-fluorouracil
Tx: Cancer Mech: _Inh. thymidylate synthatase_→inh. thymidine synth Prodrug--Pyrimidine analog
24
Zileuton
Tx: Asthma Mech: Inh. 5-lipoxygenase Blocks leukotriene synthesis *Enzyme inh.* SE: increases liver enzymes *zileutoN for eNzyme inhibitor*
24
What agents bind TNF
**Etanercept** (RA) **Infliximab** (RA,C) **Certolizumab** (RA,C) **Adalimumab** (RA) **Golimumab** (RA, etc) Think TNF=TNT (dynamite) **_E_**xplosions _In_ **_C_**aves **_A_**ffect **_Gol_**lum
25
Imitinib
Tx: Chronic myelogenous leukemia (_CML_) Mech: **Kinase inh.** In CML a gene codes for a kinase that shuts off apoptosis So cells keep multiplying and don't die=cancer Imitinib inhibits the kinase so that apoptosis occurs again Orally SE: Edema (only a few SE)
26
Prednisone
Tx: Cancer-leukemias and lymphomas Mech: Inh. immune system fxns (refer to other lecture) SE: lots of them
27
Theophylline
Tx: Asthma Mech: **Inh. cAMP PDE**→bronchodilation *Enzyme inh.* So increase in cellular cAMP Methyl xanthine like caffeine Clinical use: Chronic asthma Low TI but used now b/c very cheap SE: * Cardiac stimulation-arrythmias * CNS stim-tremors, insomnia, seizures * GI upset
28
Cyclophosphamide
Tx: Cancer Mech: _Alkylating agent_ * Add alkyl group to DNA * Causes DNA cross linking, inhibits cell replication, and RNA synth Nitrogen mustard Developed from mustard gas-destroys everything it touches Prodrug given orally or IV Stops cell from replicating once it hits DNA Lots of collateral damage
29
Ustekinumab
Ustek-i-nu-mab *MAb affecting immune sys. from human source* Immunosuppressant Tx: **Psoriasis** Mech: Binds to **IL-12, 23** * Michael Jordan _used_ to wear #_23_ until someone stole his jersey and he had to wear #_12_ (true story). Whoever stole it ought to be _sorry_.* * MJ _uste_-kinumab wear _IL-23_ then wore _IL-12_. They ought to be _psoriases._*
30
Fulvestrant
Same as Tamoxifen Tx: Cancer Mech: Blocks estrogen receptor SE: * Cataracts * Retinal changes
31
Cetirizine
Second gen H1 blocker Pharmacokinetics: Ionized in blood so fewer CNS effects Don't cause drowsiness Not metab by P450 Toxicity: * High TI * But suicide attempts b/c readily available * Anti-muscarinic effects
32
Ixabepilone
Tx: Cancer Mech: Binds to microtubules Natural product * Ixabepilone * * Pixabepilone* * Pixy sticks=tube=microtubules* * Yeah this one is a stretch...*
32
Bortezomib ## Footnote *and carfilzomib*
Tx: Multiply myeloma Mech: Proteasome/protease inh. **Enzyme inhibitors** Allows excess proteins to accumulate and kill myeloma *"Zomibs" inh. proteaZomes*
34
Ipratropium
*"-trop-" like a**_trop_**ine * Tx: Asthma Bronchodilator Mech: Cholinergic blocker Analog of atropine Clinical use: Mainly for _COPD_ but some use for asthma Kinetics: * Inhaled--slower onset though (10 min) * Not well absorbed * Peak effect in hours * Weaker than B-blockers SE: Anti-cholinergic effects​ Contraindications: * Urinary retention * Open angle glaucoma
34
Vincristine and vinblastine
Tx: Cancer Mech: Bind to microtubules and block cell mitosis Route: IV Natural product
36
Hydroxyzine
First gen H1 blocker Tx: Sedative, anti-itch Pharmacokinetics: Slightly lipid soluble, not ionized→**Gets into CNS** Toxicity: * High TI * But suicide attempts b/c readily available * Interactions w/ other CNS depressants * Anti-muscarinic effects
37
Rilonacept
Tx: RA Mech: Binds to _IL-1_ Route: SubQ Used w/ other immunosuppressants like methotrexate Should NOT be used w/ TNF inh b/c may lead to serious infection (too much suppression) * Anakinra-blocks IL1 receptor* * Rilonacept-binds to IL1*
38
Leuprolide
Tx: Cancer (prostate) Mech: _Activates GnRH receptor_ Initially increases test synth, but eventually down regulates it Used in comb. w/ other drugs *_Lou_ Ferrigno was a _pro_ bodybuilder w/ **_AR_**nold--initially boosted test. synth but eventually downregulated it* *_Leu_-_pro_-lide **_A_**ctivates GnRH **_R_**eceptor--initially boosted test. synth but eventually downregulated it*
39
Hydroxychloroquinone
Immunosuppressant Mech: * Taken up by macs and conc. in mac lysosomes * Interferes w/ mac. processing of antigens (1st step in immune process) Toxicities: * GI fxn * Dermatitis * **Irr. retinal damage** * Retinal changes and visual disturbances may progress even after discontinuation
40
Nabumetone
NSAID
42
Cromolyn sodium
*"-crom-"* Tx: Asthma Anti-inflammatory agent Mech: * Inhibit release of mediators from immune cells * Inhibits Cl channels * Inhibits Ca uptake (Ca necessary for secretion) Not bronchodilators Route: inhalation Not used much anymore
44
Belatacept
Tx: Renal transplantation Immunosuppressant Mech: binds to CD80, CD86 _receptor_ *Affects T cell activation* SE: * Increase malignancy **AB**atacept **CD**80+86 receptors (**B**elatacept too) Abatacept: RA Belatacept: Kidney trans.
46
Nedocromil
*"-crom-"* Tx: Asthma Anti-inflammatory agent Mech: * Inhibit release of mediators from immune cells * Inhibits Cl channels * Inhibits Ca uptake (Ca necessary for secretion) Not bronchodilators Route: inhalation Not used much anymore
46
Anastrazole
Tx: Cancer Mech: _Inh. aromatase_ Aromatase converts test→estr. * Ana is strong b/c aromatase inh. so test can't be converted to est. * * Ana-stro-zole. Aromatase Inh so no conversion to est.* * \*Both of the estrogen blockers have a woman's name and a reference to strength\** ***Tam-ox**-ifen* ***Ana-stro**-zole*
47
First Generation H1 blockers
**Diphenhydramine** **Clemastine** **Chloropheniramine** **Hydroxyzine** **Promethazine** **Tripelennamine**
47
Cimetidine
H2 blocker Does not cross BB barrier Effects: * Blockade of H2 receptors→**Decrease H secretion** * Histamine required to stim. acid secretion from parietal cells SE: * **Anti-androgenic effect** * Males: gynecomastia and reduced sperm count * Females: Lactation
48
Fluticasone
Tx: Asthma **DOC** for prophylaxis Mech: Bind intracellular receptor→altered DNA transcription *Activate receptor* Increase _lipocortin_→inh. synth of _phospholipase A2_ (precursor of prost and leukotriene) Route: Inhalation 1st pass metabolism SE: * Infections (esp mouth)-thrush * Dysphonia (diff. speaking) * Systemic effects
49
Budesonide
Tx: Asthma **DOC** for prophylaxis Mech: Bind intracellular receptor→altered DNA transcription *Activate receptor* Increase _lipocortin_→inh. synth of _phospholipase A2_ (precursor of prost and leukotriene) Route: Inhalation 1st pass metabolism SE: * Infections (esp mouth)-thrush * Dysphonia (diff. speaking) * Systemic effects
49
Tofacitinib
-ib=inhibitor (often kinase inh) Mech: _Janus kinase inh._ * Inh signal pathways of cytokines and ILs * Modifies effect of cytokines on gene exp * Prevents act. of signal transducers and activators of trans. SE: * Increase infection * Increase malignancy
50
Paclitaxel and other "-taxel"s
Tx: Cancer Mech: Forms abnormal microtubules Natural-from western yew tree. But now purely synthetic *"-**_t_**axels" make **_t_**errible **_t_**ubules*
50
Acetaminophen
Tx: Analgesic **Not an NSAID**--Non-narcotic analgesic No anti-platelet effect Not effective for arthritis Mech: Inh COX Toxicity: * less GI effects than ASA * OD=10-15g (20-30 tablets)-can cause irreversible liver damage * Feel bad, then better, then liver starts to fail in a few days * Decreased glutathione in liver-**treat w/ reducing agent (N-acetyl cysteine)** * Alcoholics and acetaminophen lead to decreased glutathione w/ smaller dose
52
Tacrolimus
Tx: Transplantation Immune suppression Mech: * Binds to FK binding protein * _Inh. calcineurin phosphatase _ * Like cyclosporin but binds to diff protein→inh. of cytokine synth More eff. than cyclosporin A-Increase max inh. effect SE: * Nephrotoxicity * Neurotoxicity * Alopecia (baldness) * Less cosmetic effects than cyclosporine * Diabetes Metab by P450 * Tacrolimus for transplantations* * What else binds to FK protein? Sirolimus/Everolimus* * Tacrolimus: Inh calcinuerin phosphatase* * Sirolimus: Inh kinase* * What else affects calcinuerin phosphatase? Cyclosporine* * Cyclosporine: Binds cyclophyllin* * Tacrolimus: Binds FK protein*
53
Beclomethasone
Tx: Asthma **DOC** for prophylaxis Mech: Bind intracellular receptor→altered DNA transcription *Activate receptor* Increase _lipocortin_→inh. synth of _phospholipase A2_ (precursor of prost and leukotriene) Route: Inhalation 1st pass metabolism SE: * Infections (esp mouth)-thrush * Dysphonia (diff. speaking) * Systemic effects
55
Sirolimus
Tx: Transplant, psoriasis Mech: Bind to FK binding protein _inh. kinase_ required for binding of IL-2 induced transcription factors to DNA→decreased cytokine production Often used in combination w/ glucocorticoids SE: * Some renal toxicity * Less than tacrolimus * Synergistic effect w/ used in comb w/ many immunosupp. * Some lung toxicity Metab by P450 * What else binds to FK protein? Tacrolimus* * Tacrolimus: Inh calcinuerin phosphatase* * Sirolimus/Everolimus: Inh kinase*
56
Indomethacin
NSAID Tx: Patent ductus arteriosus * Hole would not close due to excess PGs * Indomethacin would allow closure, but so does ibuprofen too Mech: Very potent COX inh. Acetic acid derivative SE: * Thrombocytopenia * Aplastic anemia * Corneal opacity
57
Basiliximab
Immunosuppressant Mech: IL-2 _receptor_ blocker Used w/ CSA 65% human (chimeric) Hypersensitivity rxn * Hypotension * Bronchospasm * Pulmonary edema **_H_**arry **_P_**otter is a _hypersensitive_ **_b_**itch when he fights the _basilisk_ in the **_C_**hamber of **_S_**ecrets, which is the **_2_**nd **_r_**eading in the series **_H_**ypotension + **_P_**ulmonary edema, _hypersensitivity_, **_b_**ronchospasm, _basiliximab_, used w/ **_CS_**A. IL-_2_ receptor blocker
57
-methasone
Dexamethasone Betamethasone Immunosuppressive potency=15 Relative minerallocorticod activity= Duration: 36-54hrs
59
Anakinra
Tx: RA Mech: Blocks IL-1 _receptor_ Route: SubQ Used w/ other immunosuppressants like methotrexate Should NOT be used w/ TNF inh b/c may lead to serious infection (too much suppression) *anakinRA=RA=RAceptor blocker*
60
Glucocorticoids
Tx: Inh. all immune processes Immunosuppressant Mech: * GC cross CM, bind to receptor and dimerize, then affect trans. * Decrease PGE and leukotrienes * Alter migration of immune cells Often used in comb. w/ other immunosuppressants SE: Sig SE w/ long term use. Refer to other lecture
61
Rituximab
Tx: Chronic lymphocytic leukemia and RA Mech: vs CD20
62
Natalizumab
Nata-li-zu-mab *MAb affecting immune sys. from humanized source* Immunosuppressant Tx: **Chron's + MS** Mech: Binds to **alpha integrin binding site** on CD4 (and other immune cells) *Not really a receptor but a "binding site"* SE: * Linked w/ progressive multifocal leukoencephalothopy (PML) * Fatal viral disease of CNS ***_Nat_**ty's give you the beer shits* ***_Nat_**alizumab=Chron's* nat**_ALI_**zumab-binds **_AL_**pha **_I_**ntegrin binding site
64
Teriflunomide
Immunosuppressant Gets converted from prodrug Leflunomide Mech: Inhibits dihydroorotate DH * Rate limiting step in production of pyrimidine (so inh. pyr. production) * Decrease in UMP and TMP * More effect on lymphocytes SE: * Diarrhea and abdominal pain (rapidly replicating GI cells) * Flu-like symptoms w/ flunomides * Teratogenic * Must take bile acid binding agent to get rid of all of drug if pregnant **Inhibits P450** * You no ride w/ me--get DD* * "Flu-no-ride w/ me. Get DD (dihydroorate DH)*
65
Leflunomide
Immunosuppressant Prodrug. Gets converted into Teriflunomide Mech: Inhibits dihydroorotate DH * Rate limiting step in production of pyrimidine (so inh. pyr. production) * Decrease in UMP and TMP * More effect on lymphocytes SE: * Diarrhea and abdominal pain (rapidly replicating GI cells) * Flu like symptoms w/ flunomides * Teratogenic * Must take bile acid binding agent to get rid of all of drug if pregnant **Inhibits P450** * You no ride w/ me--get another Designated Driver* * "Flu-no-ride w/ me. Get another DD (inh. Dihydroorate DH)*
66
Bleomycin
Tx: Cancer Mech: Intercalates w/ DNA-causes DNA strand breakage SE: pulmonary fibrosis ***_Bl_**eo**_my_**cin **_bl_**ows _my_ DNA apart* ***_Bleo_**mycin affects your ability to _blow_ (Pulmonary fibrosis)*
67
Eribulin
Tx: Cancer Mech: inh. microtubules-prevents mitosis, causes apoptosis Fully synthetic
69
Alkylating agents *Names and mech.*
Cyclophosphamide Lomustine Cisplatin Mech * Add alkyl group to DNA * Causes DNA cross linking, inhibits cell replication, and RNA synth * Non specific * Inhibit non-replicating tumor cells * Worry about extravasation-leakage into surrounding tissue
70
Celecoxib
Cele-cox-ib **Selective cox(2) inhibitor** Tx: Analgesic and anti-inflam
71
Dexamethasone
Tx: Asthma **DOC** for prophylaxis Mech: Bind intracellular receptor→altered DNA transcription *Activate receptor* Increase _lipocortin_→inh. synth of _phospholipase A2_ (precursor of prost and leukotriene) Route: _Not_ inhaled SE: * Infections (esp mouth)-thrush * Dysphonia (diff. speaking) * Systemic effects
71
Cyclosporine
Tx: Transplants, psoriasis, dry eye (tear duct inflam) Fungus derived Route: Emulsion Mech: Binds to intracellular protein-cyclophyllin Complex forms and _inh. enzyme-_calcineurin phosphatase ***Enzyme inhibitor*** Prevents act. of NFAT complex which then prevents act of gene that codes for IL2,3 and TNF alpha T cell inhibited Kinetics * Metabolized by P450 * Lots of drug interactions-esp. antibiotics SE: * Nephrotoxicity * Hepatotoxicity * Cosmetic changes * Hypertrichosis * Gingival hyperplasia * Increased cholesterol (reversible) * Mild hypertension (reversible) **C**yclosporin-binds to **C**yclophyillin→inh. **C**alcinuerin, used for **C**rusty eyes and skin, may cause **C**osmetic **C**hanges, î **C**holesterol, **C**idney (kidney) damage * What else affects calcinuerin phosphatase? Tacrolimus* * Cyclosporine: Binds cyclophyllin* * Tacrolimus: Binds FK protein*
72
Isoproterenol
"-nol"s and "-rol"s Tx: Asthma Bronchodilator--**DOC** for short term relief Mech: More specific B2 agonist than epi. but B1 effects Kinetics: Shorter T1/2 SE: * Tremors * Tachycardia * Heart palpitations *Has been supplanted by more specific B2 agonists*
73
Doxorubicin And other rubicins
Tx: Cancer Mech: Intercalates w/ DNA→blocks DNA and RNA synth Produces free radicals→break down DNA strands Class: Antibiotic (produced by microorganisms) SE: * Can cause heart m. degeneration * Irr. due to free radicals * Fall in love w/ Ruby but she's a free radical and breaks your heart.* * Rubicin. Causes free radicals--\> heart damage. Breaks DNA*
74
Famotidine
H2 blocker Does not cross BB barrier Effects: * Blockade of H2 receptors→Decrease H secretion * Histamine required to stim. acid secretion from parietal cells
75
Trastuzumab
Tx: Cancer Mech: vs HER2 Human epidermal growth factor receptor * Don't hook up w/ _her_ _too_, that's _trashy_* * Don't hook up w/ _HER2_, thats _tras_-tuzumab*
77
Second generation H1 blockers
**Loratadine** **Fexofenadine** **Desloratadine** **Cetirizine** Don't cause drowsiness Fewer CNS effects Ionized in blood **Not metab. by P450** * What does the fox say?* * What _des_ the _fex_ _ce_?* ***_Des_**loratadine (+ loratadine) **_fex_**ofenadine **_ce_**tirizine*
78
Ciclesonide
Tx: Asthma **DOC** for prophylaxis Mech: Bind intracellular receptor→altered DNA transcription *Activate receptor* Increase _lipocortin_→inh. synth of _phospholipase A2_ (precursor of prost and leukotriene) Route: Inhalation 1st pass metabolism SE: * Infections (esp mouth)-thrush * Dysphonia (diff. speaking) * Systemic effects
79
Tocilizumab
Toci-li-zu-mab *MAb affecting immune sys. from humanized source* Immunosuppressant Tx: **RA** Mech: Binds to **IL-6 _receptor_** * Football players get _tackled_ so they have _RA_ but all of the ladies want to have **_r_**isque _sex_ w/ them* * Football players get _tocilizumab_ so they have _RA_ but all the ladies want to have _IL-6_ **_r_**eceptor with them*
80
"-lukast"s
Zafirlukast Montelukast Tx: Asthma Mech: Leukotriene receptor blocker
81
Triamcinolone
Immunosuppressive potency=4 Relative minerallocorticod activity=.25 Duration: 18-36hrs
83
H2 blockers ## Footnote *Names*
*"-tidine"s* Cimetidine Ranitidine Famotidine Nizatidine *\*Only diff amongst all is that cimetidine has anti-androgenic effects*
84
Relatively selective B2 agonists
Al**_b_**ute**_rol_** Pir**_b_**ute**_rol_** **_B_**itolte**_rol_** Leval**_b_**ute**_rol_** Tert**_b_**utaline *Relatively selective are the only B2 agonists with a "b" and a "rol" (and tertButaline)* Tx: Asthma Bronchodilator--**DOC** for short term relief Mech: More specific B2 agonist than isoproterenol Kinetics: Longer T1/2=6hrs Route: Inhalation--immediate onset SE: * Tremors * Tachycardia * Heart palpitations * Fewer SE than isoproterenol but still some B1 * Downregulation of receptor * Any receptor activators may do this
84
Infliximab
Infli-xi-mab Tx: RA, Chron's Immunosuppressant Mech: Binds _TNF_ Route: IV SE: * Infusion→itching, hypertension, fever * Concerned if pt has pre-existing infection like fungus or Tb b/c infection may become worse * If you are **_inflex**_ible (from sitting on the toilet=Chron's) take _**inflix**_imab although it may lead to _**i_**tching* * May also lead to hyper**T**ensio**N** and **F**ever--binds to **TNF***
86
Lomustine
Tx: Cancer Mech: _Alkylating agent_ * Add alkyl group to DNA * Causes DNA cross linking, inhibits cell replication, and RNA synth Prodrug given IV
88
Adalimumab
Ada-li-mu-mab Tx: RA Immunosuppressant Mech: Binds _TNF_
90
Methotrexate
Tx: Cancer (and RA and psoriasis) Mech: * Analog of Folic Acid * _Inh. enzyme: Dihydrofolate reductase_ * PABA→Folic acid**⇒**Dihydrofolic acid⇒tetrahydrofolic acid * ⇒ indicate where DHFR works SE: * Myelosuppression-inh. of blood cells * Can be dealt w/ by giving _leucovorin_-THFA analog * Does not require DHFR * Will rescue "normal" cells, but not malignant cells
92
Sumatriptan and other "-triptan"s
Rizatriptan Zolmitriptan Naratriptan Almotriptan Eletriptan Frovatriptan Tx: Migraine Mech: 5HT _receptor agonist_ Route: Orally as spray Not to be used w/ SSRIs or MAO inh--will lead to synergistic effect→_5HT syndrome_→malignant hyperthermia like syndrome
93
Certolizumab
Tx: RA, Chron's Immunosuppressant Mech: Binds _TNF_
94
Ranitidine
H2 blocker Does not cross BB barrier Effects: * Blockade of H2 receptors→Decrease H secretion * Histamine required to stim. acid secretion from parietal cells
95
Pyroxicam
NSAID
97
Etodolac
NSAID
98
Aspirin
Tx: Analgesic, antipyretic, anti-inflam, anticlotting Mech: **Inh. COX** Therefore _inh. prostaglandin synth_ (and thromboxane) Kinetics: * ASA is _weak acid_ so absorbed in stomach * _Dissociates in plasma_ to form salicylic acid strongly bound to plasma proteins * 325-500mg/tablet; 4-6/day for arthritis * Lethal dose * Children(and elderly): 4g (12 tablets) * Adults 20g (50-60 tablets) * Death due to pulmonary edema SE: * GI * Slicylic acid is direct irritant * ASA decreases PG production by intestinal mucosa * Decrease mucous production * Decrease HCO3 production * CNS effects * Tinnitus (large doses) * Increase resp rates * Other effects * Don't take aspirin w/ warfarin * Direct effect on iris-decrease miosis during eye surgery * Decrease kidney perfusion * Hypersensitivity * Bronchospasms-esp in pts w/ nasal polyps * Inh. labor (PGs involved) ... ***A**sthmatic bronchospasms* ***S**evere pulmonary edema* ***P**eptic ulcer* ***I**nhibit labor* ***R**eye’s syndrome/Renal perfusion decrease* ***I**ris--Inhibit miosis* ***N**oise*
99
cytarabine
Tx: Cancer Mech: Inh. DNA polymerase Prodrug--Pyrimidine analog
100
Desloratadine
Second gen H1 blocker Pharmacokinetics: Ionized in blood so fewer CNS effects Don't cause drowsiness Not metab by P450 Toxicity: * High TI * But suicide attempts b/c readily available * Anti-muscarinic effects
101
Omalizumab
Tx: Asthma Mech: Blocks IgE receptor *Receptor blocker* Route: Injection--like all monoclonal antibodies
102
Ibuprofen ## Footnote *and other -pro-*
Naproxyn Fenoprofen Ketoprofen Flurbiprofen Oxaprozin Suprofen Tx: Analgesic, anti-inflam Mech: Inh COX Propionic acid derivative
103
Etanercept
Tx: RA Immunosuppressant Mech: Binds _TNF_ Route: SubQ (in comb. w/ other immunosupp) Synthesized molecule e**T**a**N**ercept-binds **TN**F
104
Tiotropium
*"-trop-" like a**_trop_**ine * Tx: Asthma Bronchodilator Mech: Cholinergic blocker Analog of atropine Clinical use: Mainly for _COPD_ but some use for asthma Kinetics: * Inhaled--slower onset though (10 min) * Not well absorbed * Peak effect in hours * Weaker than B-blockers SE: Anti-cholinergic effects​ Contraindications: * Urinary retention * Open angle glaucoma
105
Etoposide
Tx: Cancer Mech: Inhibits topoisomerase II→unrepairable DNA breaks Natural product * You know its a **_top_**oisomerase inhibitor but which one?* * Add the first letter of one vs two to the front. If it makes sense it's correct* * Tetoposide vs oetoposide* * \*\***T**-etoposide so topoisomerase **T**wo\*\**
106
Nizatidine ## Footnote
H2 blocker Does not cross BB barrier Effects: * Blockade of H2 receptors→Decrease H secretion * Histamine required to stim. acid secretion from parietal cells
107
Mycophenolate mofetil
Tx: Transplants and lupus More specific replacement than azothioprine _Inh. enzyme_ inosine monophosphate DH→Inh. guanisine synth. SE: Bone marrow decrease GI cell disruption
108
Cisplatin
Tx: Cancer Mech: _Alkylating agent_ * Add alkyl group to DNA * Causes DNA cross linking, inhibits cell replication, and RNA synth Contains platinum (expensive) Associated w/ renal damage and ototoxicity
110
Abiraterone
Tx: Cancer (prostate) Mech: _Inhibits 17-hydroxylase lyase_ (CYP 17) Inhibits androgen synthesis **Inhibits P450** * Get this man _a beer_, at least _17 sips_, he can't make any _androgens_.* * Get this men _abir_-aterone, _17 CYP_, can't make any _androgens_* * P450 inhibitors from this unit: Abiraterone and -flunomides*
111
Epinephrine
Tx: Asthma Bronchodilator--**DOC** for short term relief Mech: Acts on all adrenergic receptors SE * Tons of them * Increase HR+vasoconstriction→increase BP
112
Prednisone + Prednisolone
Immunosuppressive potency=4 Relative minerallocorticod activity=.25 Duration: 18-36hrs Prednisone is a prodrug: * Must be metab by P450 (in liver) * _Not effective topically_