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Pharm 4 > Unit 4 Drugs in Random Order > Flashcards

Unit 4 Drugs in Random Order Flashcards

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 acid⇒Dihydrofolic 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
Q

Atgam

A

ATGam

Tx: Acute renal transplant injection

Immunosuppressant

Antithymocyte globulin (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
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19
Q

“-fenac”s

A

diclofenac

bromfenac

Nepafenac

NSAID

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20
Q

Longer lasting relatively selective B2 agonists

A

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

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21
Q

Azathioprine

A

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

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22
Q

Diphenhydramine

A

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
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23
Q

Everolimus

A

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*
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23
Q

5-fluorouracil

A

Tx: Cancer

Mech: Inh. thymidylate synthatase→inh. thymidine synth

Prodrug–Pyrimidine analog

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24
Q

Zileuton

A

Tx: Asthma

Mech: Inh. 5-lipoxygenase

Blocks leukotriene synthesis

Enzyme inh.

SE: increases liver enzymes

zileutoN for eNzyme inhibitor

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24
Q

What agents bind TNF

A

Etanercept (RA)

Infliximab (RA,C)

Certolizumab (RA,C)

Adalimumab (RA)

Golimumab (RA, etc)

Think TNF=TNT (dynamite)

Explosions In Caves Affect Gollum

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25
Q

Imitinib

A

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)

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26
Q

Prednisone

A

Tx: Cancer-leukemias and lymphomas

Mech: Inh. immune system fxns (refer to other lecture)

SE: lots of them

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27
Q

Theophylline

A

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
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28
Q

Cyclophosphamide

A

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

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29
Q

Ustekinumab

A

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.*
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30
Q

Fulvestrant

A

Same as Tamoxifen

Tx: Cancer

Mech: Blocks estrogen receptor

SE:

  • Cataracts
  • Retinal changes
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31
Q

Cetirizine

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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32
Q

Ixabepilone

A

Tx: Cancer

Mech: Binds to microtubules

Natural product

  • Ixabepilone *
  • Pixabepilone*
  • Pixy sticks=tube=microtubules*
  • Yeah this one is a stretch…*
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32
Q

Bortezomib

and carfilzomib

A

Tx: Multiply myeloma

Mech: Proteasome/protease inh.

Enzyme inhibitors

Allows excess proteins to accumulate and kill myeloma

“Zomibs” inh. proteaZomes

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34
Q

Ipratropium

A

*“-trop-“ like atropine *

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
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34
Q

Vincristine and vinblastine

A

Tx: Cancer

Mech: Bind to microtubules and block cell mitosis

Route: IV

Natural product

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36
Q

Hydroxyzine

A

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
Q

Rilonacept

A

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
Q

Leuprolide

A

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
Q

Hydroxychloroquinone

A

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
Q

Nabumetone

A

NSAID

42
Q

Cromolyn sodium

A

“-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
Q

Belatacept

A

Tx: Renal transplantation

Immunosuppressant

Mech: binds to CD80, CD86 receptor

Affects T cell activation

SE:

  • Increase malignancy

ABatacept CD80+86 receptors (Belatacept too)

Abatacept: RA Belatacept: Kidney trans.

46
Q

Nedocromil

A

“-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
Q

Anastrazole

A

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
Q

First Generation H1 blockers

A

Diphenhydramine

Clemastine

Chloropheniramine

Hydroxyzine

Promethazine

Tripelennamine

47
Q

Cimetidine

A

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
Q

Fluticasone

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
49
Q

Budesonide

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
49
Q

Tofacitinib

A

-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
Q

Paclitaxel

and other “-taxel”s

A

Tx: Cancer

Mech: Forms abnormal microtubules

Natural-from western yew tree. But now purely synthetic

”-_t_axels” make _t_errible _t_ubules

50
Q

Acetaminophen

A

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
Q

Tacrolimus

A

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
Q

Beclomethasone

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
55
Q

Sirolimus

A

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
Q

Indomethacin

A

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
Q

Basiliximab

A

Immunosuppressant

Mech: IL-2 receptor blocker

Used w/ CSA

65% human (chimeric)

Hypersensitivity rxn

  • Hypotension
  • Bronchospasm
  • Pulmonary edema

Harry Potter is a hypersensitive bitch when he fights the basilisk in the Chamber of Secrets, which is the 2nd reading in the series

Hypotension + Pulmonary edema, hypersensitivity, bronchospasm, basiliximab, used w/ CSA. IL-_2_ receptor blocker

57
Q

-methasone

A

Dexamethasone

Betamethasone

Immunosuppressive potency=15

Relative minerallocorticod activity=

Duration: 36-54hrs

59
Q

Anakinra

A

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
Q

Glucocorticoids

A

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
Q

Rituximab

A

Tx: Chronic lymphocytic leukemia and RA

Mech: vs CD20

62
Q

Natalizumab

A

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

natALIzumab-binds ALpha Integrin binding site

64
Q

Teriflunomide

A

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
Q

Leflunomide

A

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
Q

Bleomycin

A

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
Q

Eribulin

A

Tx: Cancer

Mech: inh. microtubules-prevents mitosis, causes apoptosis

Fully synthetic

69
Q

Alkylating agents

Names and mech.

A

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
Q

Celecoxib

A

Cele-cox-ib

Selective cox(2) inhibitor

Tx: Analgesic and anti-inflam

71
Q

Dexamethasone

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
71
Q

Cyclosporine

A

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)

Cyclosporin-binds to Cyclophyillin→inh. Calcinuerin, used for Crusty eyes and skin, may cause Cosmetic Changes, î Cholesterol, Cidney (kidney) damage

  • What else affects calcinuerin phosphatase? Tacrolimus*
  • Cyclosporine: Binds cyclophyllin*
  • Tacrolimus: Binds FK protein*
72
Q

Isoproterenol

A

“-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
Q

Doxorubicin

And other rubicins

A

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
Q

Famotidine

A

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
Q

Trastuzumab

A

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
Q

Second generation H1 blockers

A

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
Q

Ciclesonide

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
79
Q

Tocilizumab

A

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 risque sex w/ them*
  • Football players get tocilizumab so they have RA but all the ladies want to have IL-6 receptor with them*
80
Q

“-lukast”s

A

Zafirlukast

Montelukast

Tx: Asthma

Mech: Leukotriene receptor blocker

81
Q

Triamcinolone

A

Immunosuppressive potency=4

Relative minerallocorticod activity=.25

Duration: 18-36hrs

83
Q

H2 blockers

Names

A

“-tidine”s

Cimetidine

Ranitidine

Famotidine

Nizatidine

*Only diff amongst all is that cimetidine has anti-androgenic effects

84
Q

Relatively selective B2 agonists

A

Albuterol

Pirbuterol

Bitolterol

Levalbuterol

Tertbutaline

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
Q

Infliximab

A

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 hyperTensioN and Fever–binds to TNF*
86
Q

Lomustine

A

Tx: Cancer

Mech: Alkylating agent

  • Add alkyl group to DNA
  • Causes DNA cross linking, inhibits cell replication, and RNA synth

Prodrug given IV

88
Q

Adalimumab

A

Ada-li-mu-mab

Tx: RA

Immunosuppressant

Mech: Binds TNF

90
Q

Methotrexate

A

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
Q

Sumatriptan

and other “-triptan”s

A

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
Q

Certolizumab

A

Tx: RA, Chron’s

Immunosuppressant

Mech: Binds TNF

94
Q

Ranitidine

A

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
Q

Pyroxicam

A

NSAID

97
Q

Etodolac

A

NSAID

98
Q

Aspirin

A

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)

…

Asthmatic bronchospasms

Severe pulmonary edema

Peptic ulcer

Inhibit labor

Reye’s syndrome/Renal perfusion decrease

Iris–Inhibit miosis

Noise

99
Q

cytarabine

A

Tx: Cancer

Mech: Inh. DNA polymerase

Prodrug–Pyrimidine analog

100
Q

Desloratadine

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
101
Q

Omalizumab

A

Tx: Asthma

Mech: Blocks IgE receptor

Receptor blocker

Route: Injection–like all monoclonal antibodies

102
Q

Ibuprofen

and other -pro-

A

Naproxyn

Fenoprofen

Ketoprofen

Flurbiprofen

Oxaprozin

Suprofen

Tx: Analgesic, anti-inflam

Mech: Inh COX

Propionic acid derivative

103
Q

Etanercept

A

Tx: RA

Immunosuppressant

Mech: Binds TNF

Route: SubQ (in comb. w/ other immunosupp)

Synthesized molecule

eTaNercept-binds TNF

104
Q

Tiotropium

A

*“-trop-“ like atropine *

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
Q

Etoposide

A

Tx: Cancer

Mech: Inhibits topoisomerase II→unrepairable DNA breaks

Natural product

  • 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*
  • Tetoposide vs oetoposide*
  • **T-etoposide so topoisomerase Two***
106
Q

Nizatidine

A

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
Q

Mycophenolate mofetil

A

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
Q

Cisplatin

A

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
Q

Abiraterone

A

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
Q

Epinephrine

A

Tx: Asthma

Bronchodilator–DOC for short term relief

Mech: Acts on all adrenergic receptors

SE

  • Tons of them
  • Increase HR+vasoconstriction→increase BP
112
Q

Prednisone

+

Prednisolone

A

Immunosuppressive potency=4

Relative minerallocorticod activity=.25

Duration: 18-36hrs

Prednisone is a prodrug:

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

Pharm 4 (9 decks)

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