Unit 4 Drugs in Random Order Flashcards
Bevacizumab
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
Dactinomycin
Tx: Cancer
Mech: Intercalates w/ DNA and interferes w/ mRNA synth
Tripelennamine
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
Fexofenadine
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
Prednisone
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
Abatacept
Tx: RA
Immunosuppressant
Mech: binds to and inh. CD80, CD86 receptors
Affects T cell activation
ABatacept CD80+86 receptors
_A_batacept for _A_rthritis
Ibritumomab
Tx: Cancer
Mouse MAB
Severe infusion rxn
Sulindac
NSAID
Acetic acid derivative
Tamoxifen
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
Topotecan
and irinotecan
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***
Flutamide
and other “lutamides”
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*
Other NSAIDs
_Pyr_os _ne_ed _e_xcess _f_ire
_Pyr_oxicam _n_abumetone _e_todolac -_f_enac
6-mercaptopurine
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*
Acetic acid derived NSAIDs
Double A (Aaron) slobbers into titties
Acetic Acid: Sulindac indomethacin tolmetin
Methotrexate
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
- Inh. lots of folic acid dependent processes, especially in cells w/ rapid turnover (at high doses):
Clemastine
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
Promethazine
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
Chlorpheniramine
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
Cortisone
+
Hydrocortisone
Immunosuppressive potency=1
Relative minerallocorticod activity=1
Duration: 8-12hrs
Cortisone is a prodrug:
- Must be metab by P450 (in liver)
- Not effective topically
“-ergotamine”s
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
Loratadine
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
Mometasone
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
Golimumab
Tx: RA, Ulcerative colitis, psoriatic arthritis
Immunosuppressant
Mech: Binds TNF
Tolmetin
NSAID
Acetic acid derivative
Atgam
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
“-fenac”s
diclofenac
bromfenac
Nepafenac
NSAID
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
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
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
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*
5-fluorouracil
Tx: Cancer
Mech: Inh. thymidylate synthatase→inh. thymidine synth
Prodrug–Pyrimidine analog
Zileuton
Tx: Asthma
Mech: Inh. 5-lipoxygenase
Blocks leukotriene synthesis
Enzyme inh.
SE: increases liver enzymes
zileutoN for eNzyme inhibitor
What agents bind TNF
Etanercept (RA)
Infliximab (RA,C)
Certolizumab (RA,C)
Adalimumab (RA)
Golimumab (RA, etc)
Think TNF=TNT (dynamite)
Explosions In Caves Affect Gollum
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)
Prednisone
Tx: Cancer-leukemias and lymphomas
Mech: Inh. immune system fxns (refer to other lecture)
SE: lots of them
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
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
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.*
Fulvestrant
Same as Tamoxifen
Tx: Cancer
Mech: Blocks estrogen receptor
SE:
- Cataracts
- Retinal changes
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
Ixabepilone
Tx: Cancer
Mech: Binds to microtubules
Natural product
- Ixabepilone *
- Pixabepilone*
- Pixy sticks=tube=microtubules*
- Yeah this one is a stretch…*
Bortezomib
and carfilzomib
Tx: Multiply myeloma
Mech: Proteasome/protease inh.
Enzyme inhibitors
Allows excess proteins to accumulate and kill myeloma
“Zomibs” inh. proteaZomes
Ipratropium
*“-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
Vincristine and vinblastine
Tx: Cancer
Mech: Bind to microtubules and block cell mitosis
Route: IV
Natural product
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
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*
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
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
Nabumetone
NSAID
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
Belatacept
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.
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
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
First Generation H1 blockers
Diphenhydramine
Clemastine
Chloropheniramine
Hydroxyzine
Promethazine
Tripelennamine
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
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
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
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
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
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
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*
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
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*
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
Basiliximab
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
-methasone
Dexamethasone
Betamethasone
Immunosuppressive potency=15
Relative minerallocorticod activity=
Duration: 36-54hrs
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
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
Rituximab
Tx: Chronic lymphocytic leukemia and RA
Mech: vs CD20
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
natALIzumab-binds ALpha Integrin binding site
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)*
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)*
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)
Eribulin
Tx: Cancer
Mech: inh. microtubules-prevents mitosis, causes apoptosis
Fully synthetic
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
Celecoxib
Cele-cox-ib
Selective cox(2) inhibitor
Tx: Analgesic and anti-inflam
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
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)
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*
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
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*
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
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*
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
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
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 risque sex w/ them*
- Football players get tocilizumab so they have RA but all the ladies want to have IL-6 receptor with them*
“-lukast”s
Zafirlukast
Montelukast
Tx: Asthma
Mech: Leukotriene receptor blocker
Triamcinolone
Immunosuppressive potency=4
Relative minerallocorticod activity=.25
Duration: 18-36hrs
H2 blockers
Names
“-tidine”s
Cimetidine
Ranitidine
Famotidine
Nizatidine
*Only diff amongst all is that cimetidine has anti-androgenic effects
Relatively selective B2 agonists
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
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 hyperTensioN and Fever–binds to TNF*
Lomustine
Tx: Cancer
Mech: Alkylating agent
- Add alkyl group to DNA
- Causes DNA cross linking, inhibits cell replication, and RNA synth
Prodrug given IV
Adalimumab
Ada-li-mu-mab
Tx: RA
Immunosuppressant
Mech: Binds TNF
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
- Can be dealt w/ by giving leucovorin-THFA analog
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
Certolizumab
Tx: RA, Chron’s
Immunosuppressant
Mech: Binds TNF
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
Pyroxicam
NSAID
Etodolac
NSAID
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)
…
Asthmatic bronchospasms
Severe pulmonary edema
Peptic ulcer
Inhibit labor
Reye’s syndrome/Renal perfusion decrease
Iris–Inhibit miosis
Noise
cytarabine
Tx: Cancer
Mech: Inh. DNA polymerase
Prodrug–Pyrimidine analog
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
Omalizumab
Tx: Asthma
Mech: Blocks IgE receptor
Receptor blocker
Route: Injection–like all monoclonal antibodies
Ibuprofen
and other -pro-
Naproxyn
Fenoprofen
Ketoprofen
Flurbiprofen
Oxaprozin
Suprofen
Tx: Analgesic, anti-inflam
Mech: Inh COX
Propionic acid derivative
Etanercept
Tx: RA
Immunosuppressant
Mech: Binds TNF
Route: SubQ (in comb. w/ other immunosupp)
Synthesized molecule
eTaNercept-binds TNF
Tiotropium
*“-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
Etoposide
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***
Nizatidine
H2 blocker
Does not cross BB barrier
Effects:
- Blockade of H2 receptors→Decrease H secretion
- Histamine required to stim. acid secretion from parietal cells
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
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
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*
Epinephrine
Tx: Asthma
Bronchodilator–DOC for short term relief
Mech: Acts on all adrenergic receptors
SE
- Tons of them
- Increase HR+vasoconstriction→increase BP
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
