Exam 1 Drugs Compilation Flashcards
Cimetidine
Imidazole
Inhibitor of CYP enzymes (Phase 1), competitive inhibitor of OCT
n/a for now
Decrease metabolism / increase drug level
Phenobarbital
Barbiturate
Activator of CYP enzymes (Phase 1)
n/a for now
Increase metabolism, decrease drug level
Probenecid
n/a
competitive inhibitor of OAT
n/a
Decreases secretion of anions
Ethanol
n/a
Activator of CYP enzymes
Increase metabolism, decrease drug level
Proadifen
n/a
Only known role is as inhibitor of CYPs
Decrease metabolism / increase drug level
Bethanechol
Muscarinic Receptor Agonist Muscarinic receptor selective Long acting Used to stimulate smooth muscle post-op (Flushing, sweating, abdominal cramps, belching, bladder tightness, headache, salivation)
Carbachol
Muscarinic Receptor Agonist
Long acting
Corneal Application for Wide Angle Glaucoma (Increase drainage)
(Flushing, sweating, abdominal cramps, belching, bladder tightness, headache, salivation)
Methacholine
Muscarinic Receptor Agonist
Muscarinic receptor selective
Used to test muscarinic receptor function, slow HR and test bronchial hyperactivity
(Flushing, sweating, abdominal cramps, belching, bladder tightness, headache, salivation)
Muscarine
Muscarinic Receptor Agonist
Muscarinic Receptor selective
(Flushing, sweating, abdominal cramps, belching, bladder tightness, headache, salivation)
Pilocarpine
Muscarinic Receptor Agonist (Natural Alkaloid)
Corneal Application for Wide Angle Glaucoma (increase drainage)
Muscarinic Receptor selective, sweat glands sensitive
(Flushing, sweating, abdominal cramps, belching, bladder tightness, headache, salivation)
Nicotine
Nicotinic Receptor Agonist
Competitive Nicotinic Receptor Agonist
Can cause Autonomic hyperactivity (convulsions, coma, death, respiratory arrest)
Varenicline
Nicotinic Receptor Agonist
Agonist
Used to quit smoking
Ambemonium
Competitive AChE inhibitor
Used to treat myasthenia gravis
(Flushing, sweating, abdominal cramps, belching, bladder tightness, headache, salivation)
Edrophonium
Quaternary Simple Alcohol
Competitive AChE inhibitor
Used to diagnose Myesthenia Gravis
(Flushing, sweating, abdominal cramps, belching, bladder tightness, headache, salivation)
Neostigmine
Carbamate
Competitive AChE inhibitor
Increases smooth muscle motility, treat paralytic ileus and atony of bladder, treatment and diagnosis of myasthenia gravis, reversal of neuromuscular block
** Used to compete off N2 receptor blockers **
(Flushing, sweating, abdominal cramps, belching, bladder tightness, headache, salivation)
Physostigmine
Carbamate
Competitive AChE inhibitor
Topical treatment for wide angle glaucoma
(Flushing, sweating, abdominal cramps, belching, bladder tightness, headache, salivation)
Pyridostigmine
Carbamate
Competitive AChE inhibitor
Treatment of myesthenia gravis, pretreatment for nerve gas exposure, reversal of neuromuscular blockade
(Flushing, sweating, abdominal cramps, belching, bladder tightness, headache, salivation)
diisopropylfluorophosphate
Organophosphate Derivative
Non - Competitive AChE inhibitor
No clinical use
SLUD
echothiophate
Organophosphate Derivative
Non - Competitive AChE inhibitor
Treatment of glaucoma
SLUD
Carbaryl
Insecticide Carbaryl
Non - Competitive AChE inhibitor
No clinical use
SLUD
Malathion
Insecticide Organophosphate Derivative
Non - Competitive AChE inhibitor
Least toxic – used for head lice
SLUD
Parathion
Organophosphate Derivative
Non - Competitive AChE inhibitor
No clinical use
SLUD
Tetraethylpyrophosphate
Insecticide Organophosphate Derivative
Non - Competitive AChE inhibitor
No clinical use
SLUD
Sarin
Nerve Gas - Organophosphate Derivative
Non - Competitive AChE inhibitor
No clinical use
SLUD
Soman
Nerve Gas - Organophosphate Derivative
Non - Competitive AChE inhibitor
No clinical use
SLUD
Pralidoxime
AchE reactivator
Releases phosphoryl moiety to restore AChE activity
Needs to be admin with Atropine, before Aging
Atropine
Muscarinic (selective) Antagonist (Long lasting)
Treatment of insecticide poisoning, anti-parkinson, cause mydriasis and cycloplegia, anti-motion sickness, decreased bronchial secretions, slow smooth muscle, Increase HR, Preanesthetic
Can cause hallucinations and amnesia
Atropine fever, dry mouth
Homatropine
Muscarinic antagonist (Intermediate lasting)
Used to cause mydriasis and cycloplegia
Can cause hallucinations and amnesia, dry mouth, sedation / excitement
Scopolamine
Muscarinic antagonist
Anti-motion sickness, Amnesia before surgery
Can cause hallucinations and amnesia, dry mouth, sedation / excitement
Methscopolamine
Muscarinic antagonist
Slow GI tract
Trihexyphenidyl
Muscarinic antagonist
Antiparkinson therapy, reduce uncoord. Movt.
Can cause hallucinations and amnesia, dry mouth, sedation / excitement
Tropicamide
Muscarinic antagonist (Short acting) Used to cause mydriasis and cycloplegia
Cyclopentolate
Muscarinic antagonist
Used to cause mydriasis and cycloplegia
Ipratropium
Muscarinic antagonist (Quaternary)
Bronchodilation, Decreased bronchial secretions,
Shorter acting for COPD
Tiotropium
Muscarinic antagonist (Quaternary)
Bronchodilation, Decreased bronchial secretions
Longer acting for COPD
Darifenacin
Muscarinic antagonist (M3 Specific)
Slow Smooth muscle, over active bladder (GI / Genitourinary)
Longer Duration of action
Solifenacin
Muscarinic antagonist (M3 Specific)
Slow Smooth muscle, over active bladder (GI / Genitourinary)
Longer Duration of action
Tolterodine
Muscarinic antagonist (M3 Specific)
Slow Smooth muscle, over active bladder (GI / Genitourinary)
Longer Duration of action
Mecamylamine
Ganglionic Blocker
Non-depolarizing competitive antagonist
Good GI absorption
Adjunct for peripheral vascular disease – relieve vasoconstriction and increase perfusion
CNS side effects including tremors, confusion, seizures, mania, depression
Trimethaphan
Ganglionic Blocker
Non-depolarizing competitive antagonist
Used IV in OR to decrease BP to control bleeding, adjunct anti-hypotensive
Succinylcholine
Non-Competitive Nicotinic N2 blocker
Depolarizing – Prevent Depolarization
Causes muscle relaxation, e.g. before surgery
Hydrolyzed by plasma cholinesterase
Curare (t-tubocurarine)
benzylisoquinolines
Competitive Nicotinic N2 blocker (N2 Specific)
Non-depolarizing – Prevent Depolarization
Causes muscle relaxation, e.g. before surgery
* Long acting *
Histamine Release (hypotension) is side effect
Reversed by edrophonium, neostigmine
Atracurium
benzylisoquinolines
Competitive Nicotinic N2 blocker (N2 Specific)
Non-depolarizing – Prevent Depolarization
Causes muscle relaxation, e.g. before surgery
* Intermediate acting *
Histamine Release (hypotension) is side effect
Reversed by edrophonium, neostigmine
Cisatracurium
benzylisoquinolines
Competitive Nicotinic N2 blocker (N2 Specific)
Non-depolarizing – Prevent Depolarization
Causes muscle relaxation, e.g. before surgery
* Intermediate acting *
Histamine Release (hypotension) is side effect
Reversed by edrophonium, neostigmine
Mivacurium
benzylisoquinolines
Competitive Nicotinic N2 blocker (N2 Specific)
Non-depolarizing – Prevent Depolarization
Causes muscle relaxation, e.g. before surgery
* Short acting *
Histamine Release (hypotension) is side effect
Reversed by edrophonium, neostigmine
Pancuronium
Ammonio Steroids
Competitive Nicotinic N2 blocker
Non-depolarizing – Prevent Depolarization
Causes muscle relaxation, e.g. before surgery
* Long acting *
Cross react with Muscarinic and N1 – Tachycardia
Reversed by edrophonium, neostigmine
Vecuronium
Ammonio Steroids
Competitive Nicotinic N2 blocker
Non-depolarizing – Prevent Depolarization
Causes muscle relaxation, e.g. before surgery
* Intermediate acting *
Cross react with Muscarinic and N1 – Tachycardia
Reversed by edrophonium, neostigmine
Metaraminol
Alpha-1 Selective Agonist
Long acting beta 1 and alpha 1 stimulant
Displaces NE
Methoxamine
Alpha-1 Selective Agonist (less alpha 2)
treat hypotensive crisis
Phenylephrine
Alpha-1 Selective Agonist (less alpha 2)
Vasoconstriction, prevent shock, nasal decongestant, treat hypotensive crisis, reduce drug diffusion, reduce mucus membrane congestion, mydriasis
Long acting
Alpha methyldopa
Alpha-2 Selective Agonist
Decrease NT in synapse – replaces DOPA in synthetic pathway to yield Alpha-methyl norepinephrine (false neurotransmitter)
Used to treat hypertension – acts at brainstem vasomotor center
Side effects diminish over time – sedation, xerostomia, anorexia, fluid retention, vivid dreams, impotence, CNS stimulation
Clonidine
Alpha-2 Selective Agonist (less alpha 1)
Decrease NT in synapse (inhibit NE release)
Side effects diminish over time – sedation, xerostomia, anorexia, fluid retention, vivid dreams, CNS stimulation
Guanabenz
Alpha-2 Selective Agonist
Decrease NT in synapse (inhibit NE release)
Side effects diminish over time – sedation, xerostomia, anorexia, fluid retention, vivid dreams, CNS stimulation
Amphetamine
Alpha and beta adrenergic agonist Releasing agent (increases NE release), also releases intraneuronal NE – reverse transport
Ephedrine
Alpha and beta adrenergic agonist
Releasing agent, Stimulant of most adrenergic receptors
Increase CO and arterial pressure, treat orthostatic hypotension, reduce mucus membrane congestion, stress incontinence
Long acting – Displaces NE
Epinephrine
Alpha and beta adrenergic agonist
Binds all adrenergic receptors equally
Potent vasoconstrictor and cardiac stimulant, hemostasis during surgery, reduce drug diffusion, anaphylaxis
Norepinephrine
Alpha and beta adrenergic agonist (except beta 2)
IV infusion for shock, increase CO and cause vasoconstriction (increase BP, treat hypotensive crisis), reduce drug diffusion
Binds Beta-2 a lot less than all other adrenergics
Dobutamine
Beta 1 Selective agonist (Less beta-2)
Cardiogenic shock, heart failure
Isoproterenol
Beta 1 and 2 agonist
Used for relaxation of bronchial smooth muscle, also cardiac stimulation (potent vasodilator)
Albuterol
Beta 2 Selective agonist (Less beta-1)
Bronchial asthma
Metaproterenol
Beta 2 Selective agonist (Less beta-1)
Bronchial asthma
Terbutaline
Beta 2 Selective agonist (Less beta-1)
Bronchial asthma, relax pregnant uterus
Bromocriptine
Dopamine Agonist
Anti-parkinson agent (for its CNS effects)
Side effects – postural hypotension and cardiac arrhythmia
Dopamine
Dopamine Agonist
IV for shock, vasoconstriction, increase CO and dilate renal arteries
Binds Alpha and Beta 1 at high concentrations
Enhance NE release (displaces it)
Fenoldopam
Dopamine Agonist, DA-1 selective
Vasodilation of renal and mesenteric vessels
Doxazosin
Alpha-1 Selective antagonist
Urinary obstruction from BPH
Prazosin
Alpha-1 Selective antagonist (Highly selective)
Antihypertensive (mild / moderate), urinary obstruction from BPH
Little to no tachycardia because doesn’t bind beta receptors
Oral admin
Tamsulosin
Alpha-1 Selective antagonist
Urinary obstruction from BPH
Terazosin
Alpha-1 Selective antagonist
Urinary obstruction from BPH
Phenoxybenzamine
Alpha-1 and Alpha-2 Selective antagonist
Non-competitive – alkylates alpha receptors (~24 hrs)
Can cause postural hypotension and tachycardia – due to decreased MAP
Used to treat hypertension associated with pheochromocytoma
Phentolamine
Alpha-1 and Alpha-2 Selective antagonist
Competitive antagonist
Dirty drug, binds histamine and muscarinic receptors
Diagnostic for pheochromocytoma, also for its assoc. hypertension
Increases NE release, will cause tachycardia and increased CO
Labetalol
Alpha and beta antagonist (more beta though)
Atenolol
Beta-1 Selective antagonist
Antihypertensive, inhibit cardiac output
** better, but still careful with asthma / COPD patients **
Doesn’t cross CNS well
Betaxolol
Beta-1 Selective antagonist
Major use – glaucoma
(antihypertensive, inhibit cardiac output – if it gets there)
** better, but still careful with asthma / COPD patients **
Metoprolol
Beta-1 Selective antagonist
Antihypertensive, angina pectoris, inhibit cardiac output
Prevent recurrence of MI
** better, but still careful with asthma / COPD patients **
Side effect – Ataxia and dizziness
Nadolol
Beta-1 and beta-2 Selective antagonist Very long acting, antihypertensive Prevent recurrence of MI **Careful with asthma and COPD patients ** Doesn’t cross CNS well
Pindolol
Beta-1 and beta-2 Selective antagonist
Antihypertensive
Prevent recurrence of MI
**Careful with asthma and COPD patients **
Propranolol
Beta-1 and beta-2 Selective antagonist
Antihypertensive, anti arrhythmic, anti-migraine, for angina pectoris
Prevent recurrence of MI
**Careful with asthma and COPD patients **
Side effect – Ataxia and dizziness
Timolol
Beta-1 and beta-2 Selective antagonist
Lower intraocular pressure, Antihypertensive, angina pectoris
Prevent recurrence of MI
**Careful with asthma and COPD patients **
Guanethidine
Synaptic vesicle depleting agent / membrane stabilizer
Used for only the most severe cases of hypertension
Enters neurons via amine 1 transporter (drugs that interfere will block its actions)
Minimal CNS effects – doesn’t cross BBB
Reserpine
Synaptic vesicle depleting agent
Blocks transport of NE into the vesicle, reduces amount released
Long duration of action
Side effects – Sedation, depression, Parkinsonism, increased GI motility (ulcers)
Cocaine
Amine 1 transport inhibitor
No clinical use – vasoconstriction, mydriasis and tachycardia
Interferes with reserpine (Amine 1 transporter)
DMI - desmethylimipramine
Tricyclic antidepressant
Amine 1 transport inhibitor
Increases NT in synapse
Tyramine
Releasing Agent (Displaces NE) Enhance NE release via Amine 1 transporter
Pseudoephedrine
Releasing Agent
Reduces congestion of mucus membranes
Dipivefrin
Alpha and beta blocker
Used for eye, metabolized to epinephrine
Apraclonidine
Alpha 2 selective agonist
Carteolol
Beta 1 and 2 antagonist
Reduce aqueous humor production in eye
Levobunolol
Beta 1 and 2 antagonist
Reduce aqueous humor production in eye
Metipranolol
Beta 1 and 2 antagonist
Reduce aqueous humor production in eye
Acetazolamide
Carbonic Anhydrase inhibitor
Reduce aqueous humor production in eye (via reducing HCO3 production)
Dichlorphenamide
Carbonic Anhydrase Inhibitor
Reduce aqueous humor production in eye (via reducing HCO3 production)
Dorzolamide
Carbonic Anhydrase Inhibitor
Reduce aqueous humor production in eye (via reducing HCO3 production)
Botulinum toxin A
Muscle Relaxant
Long term – Inhibits NT release by destroying presynaptic SNAP25
Azathioprine
- General Growth Inhibitors
- ## Metabolized to 6-mercaptopurine then 6 thioguanine (blocks purine synthesis). Also incorporates into DNA
- Inactivated by xanthine oxidase
- ## Myelosuppression, nausea, vomiting
- Used for renal and other tissue transplantation, autoimmune disease
Cyclophosphamide
-General Growth Inhibitors
-Cross links DNA, kills all proliferating cells
-
-
- Myelosuppression, nausea, vomiting,
- Infertility
- Used for autoimmune diseases, bone marrow transplant
Leflunomide
- General Growth Inhibitors
- ## Decreases pyrimidine synthesis-
- ## Diarrhea, modest hepatotoxicity, reduced myelosuppresion
- Used for Rheumatoid arthritis, some autoimmune disease
Methotrexate
-General Growth Inhibitors
- Inhibits dihydrofolate reductase, prevents thymidide and purine synthesis
-
-
- Causes nausea, mucosal ulcers, modest hepatotoxicity, reduced myelosuppression
-
- Rheumatoid arthritis, some autoimmune disease
Mycophenolate Mofetil
-General Growth Inhibitors
- Prevents Purine synthesis
-
-
- Myelosuppression, nausea, vomiting
-
- Used for solid organ transplant (cyclosporine alternative) autoimmune disease
Prednisone
-Glucocorticoid
-Upregulates / Downregulates expression of genes assoc. with inflammation and immunosuppression (e.g. IL2 and IFN-gamma)
- No serious bone marrow toxicity
-
-
- Cushings syndrome, osteoporosis, glucose intolerance, hypertension, susceptibility to infection
- Used for solid organ transplantation (first line), stem cell transplantation, autoimmune diseases, asthma, allergic reactions, systemic inflammation
Sirolimus
- mTOR inhibitor
- ## Binds FKBP12 to form complex that inhibits IL2 activation
- Antagonizes tacrolimus, synergistic with cyclosporine
- Myelosuppression, hyperlipidemia, hypertension, edema, hepatotoxicity
- Solid organ transplants, steroid resistant graft v. host disease
Cyclosporin
- Calcineurin inhibitor
- ## Binds Cyclophilin to form complex that inhibits NFAT activation
- Often combined with other immunosuppressant agents
- Nephrotoxicity, hypertension, hyperglycemia, liver dysfunction.
- Increased cancer incidence documented
- Kidney, liver and cardiac transplants, inflammatory diseases (asthma)
Tacrolimus
- Calcineurin inhibitor
- ## Binds FKBP12 to form complex that inhibits NFAT activation
- 10-100 X more potent than cyclosporine
- Nephrotoxicity, hypertension, hyperglycemia, liver dysfunction.
- Increased cancer incidence documented
- Kidney, liver and cardiac transplants, inflammatory diseases (asthma)
Anti-T cell globulin
- Antibody / Fusion Protein
- Blocks T cell surface receptors and opsonizes T cells
- Product of repeated injection of human T cells into animals
- Cytokine release syndrome (reduce w/ pretreat. With acetaminophen and antihistamine, serum sickness
- Anaphylaxis potential (with repeat use)
- Prevent maternal (Rh-) from attacking fetus
Alemtuzumab
- Antibody / Fusion Protein
- Depletes cells expressing CD25 (T and B cells, monocytes, macrophages, NK cells)
- Prolonged depletion (1 yr) of T cells and other immunecells
- Myelosuppresion, flu like symptoms
- -
Basiliximab (Anti CD25)
- Antibody / Fusion Protein
- Blocks and opsonizes alpha chain of IL-2 (CD25), found only on activated T cells
- Depletes only antigen activated T cell , reduced incidence of infection and malignancy
- Moderate effect relative to anti-T cell globulin
- Well tolerated
- -
Rh(D) immune globulin
- Antibody / Fusion Protein
- ## Binds and clears up D-antigen, prevents mother’s immune rxn
- Prevent maternal (Rh-) from attacking fetus
Belatacept
- Antibody / Fusion Protein
- ## Binds and clears up D-antigen, prevents mother’s immune rxn
- Comparable to calcineurin inhibitors in preventing transplant rejection
- Anemia, neutropenia, peripheral edema
- Increased risk of infection and malignancy, especially post-transplant lymphoproliferative disorder
- Use for kidney transplant
Interleukin-2
- Cytokines
- ## Increases proliferation of activated T cells, increases IFN-gamma and cytotoxic killer cell activity
- Capillary leak syndrome, hypotension, reduced organ perfusion, can be fatal
- Used to treat metastatic melanoma, renal cell carcinoma
IFN-gamma
- Cytokines
- ## Stimulates activity of cytotoxic cells-
-
- - Severe recurrent infections
BCG
-Adjuvant
- Increases APC activity by binding pattern recognition receptors
- Live attenuated bacillus calmette-guerin
- Can’t use systemically, will cause septic shock
-
-
- Used topically for bladder cancer
Cetirizine
- H1 antihistamines
- Second generation antihistamine
- Poor CNS Penetration
- ## Increased selectivity at H1 receptors-
- Antihistamine
Cyclizine
H1 antihistamines
- First generation antihistamine
-CNS permeable
- Non-specific effects at adrenoreceptors, muscarinics, serotonin and sodium channels
- Drowsiness
-
- Anti-histamine (allergy, uticaria), motion sickness
Dimenhydrinate
H1 antihistamines
- First generation antihistamine
- CNS permeable
-Non-specific effects at adrenoreceptors, muscarinics, serotonin and sodium channels
- Drowsiness
-
-Anti-histamine (allergy, uticaria), motion sickness
Diphenhydramine
H1 antihistamines
- First generation antihistamine
- CNS permeable
- Non-specific effects at adrenoreceptors, muscarinics, serotonin and sodium channels
- Drowsiness
-
- Anti-histamine (allergy, uticaria), motion sickness
Fexofenadine
- H1 antihistamines
- Second generation antihistamine
- Poor CNS Penetration
- ## Increased selectivity at H1 receptors-
- Antihistamine
Loratidine
- H1 antihistamines
- Second generation antihistamine
- Poor CNS Penetration
- ## Increased selectivity at H1 receptors-
- Antihistamine
Promethazine
H1 antihistamines
- First generation antihistamine
- CNS permeable
- Non-specific effects at adrenoreceptors, muscarinics, serotonin and sodium channels
- Drowsiness
-
- Anti-histamine (allergy, uticaria), antiemetic
Adalimumab
- anti-TNFalpha agent
- Binds to TNFalpha, prevents it from binding to its receptor and reduces circulating levels
- Human antibody to TNFalpha
- Parenteral administration required
- increased frequency of infections (upper
respiratory, urinary)
-
-Rheumatoid arthritis, Crohn’s
Etanercept
- anti-TNFalpha agent
- Binds to TNFalpha, prevents it from binding to its receptor and reduces circulating levels
- Fusion protein containing the ligand binding domain of the
TNFalpha receptor and the Fc domain of human IgG. - Parenteral administration required
- increased frequency of infections (upper
respiratory, urinary)
-
-Rheumatoid arthritis, Crohn’s
Infliximab
anti-TNFalpha agent - Binds to TNFalpha, prevents it from binding to its receptor and reduces circulating levels - Humanized antibody to TNFalpha - Parenteral administration required - increased frequency of infections (upper respiratory, urinary) - -Rheumatoid arthritis, Crohn's
Anakinra
- Anti-IL1 agent
- ## Competitive IL-1 receptor antagonist (IL-1Ra analog)
- Short half-life, daily injection required
Increased susceptibility to infection
- - Rheumatoid Arthritis, possibly other inflammatory diseases
Tofacitinib
- Jak kinase inhibitor
- Inhibits all activity of cytokines required for adaptive immunity (eg., IL-2, IL-4, etc.) and inhibits all activities for many inflammatory cytokines (eg., IL-6)
Distinguishing Chem Characteristics (Unique or “weird” features) - oral administration; therapeutic doses chosen to produce incomplete Jak inhibition, because higher doses expected to produce potent
immunosuppression AND adverse effects. - ## Anemia, neutropenia, general myelosuppression, increased risk of infection (especially Herpes Zoster)
- RA: Currently second line therapy for those failing methotrexate
Aspirin
Nonselective COX inhibitor
- Irreversible Acetylation of COX enzymes
- Long lasting block
-
-
-Increased bleeding, gastric ulcers, salicylism, Reye’s syndrome, dyspepsia, renal issues
- OTC analgesic / antipyretic, cardiovascular prophylaxis
Diclofenac
Nonselective COX inhibitor - Reversible inhibition of COX - - Selectivity for COX 2 over COX 1 - - Increased bleeding, gastric ulcers, dyspepsia, renal issues, CV events - RX for arthritis, anti-inflammatory
Diclofenac with misoprostol
Nonselective COX inhibitor - Reversible inhibition of COX - - Selectivity for COX 2 over COX 1 - Misoprostol should help GI symptoms - Increased bleeding, gastric ulcers, dyspepsia, renal issues, CV events - RX for arthritis, anti-inflammatory
Ibuprofen
Nonselective COX inhibitor - Reversible inhibition of COX - - -Increased bleeding, gastric ulcers. dyspepsia, renal issues, CV events - - OTC analgesic, antipyretic,
Indomethacin
Nonselective COX inhibitor
- Reversible inhibition of COX
-
- Increased inhibition of COX 1 over COX 2
-
- High incidence of GI problems leading to intolerance
- RX for arthritis, anti inflammatory
Ketorolac
Nonselective COX inhibitor - Reversible inhibition of COX - - Increased inhibition of COX 1 over COX 2 - - -Post surgical analgesic
Naproxen
Nonselective COX inhibitor
- Reversible inhibition of COX
-
-
-Increased bleeding, gastric ulcers, dyspepsia, renal issues, CV events
-
- OTC analgesic, antipyretic, RX anti-inflammatory
Acetaminophen
Nonselective COX inhibitor - - - -hepatotoxicity with overdose - -
Celecoxib
Cox-2 selective inhibitor - - - -Renal toxicity, increased risk of cardiovascular events - -
Rofecoxib
Cox-2 selective inhibitor - - - -Renal toxicity, increased risk of cardiovascular events - -
Albuterol
-Beta-2 agonist
-stim adenyl cyclase and cAMP–>relax bronch smooth m.
-
-short DOA
-tachycardia, muscle tremor, headache
-bronchodilate acute asthma
Salmeterol
-Beta-2 agonist
-stim adenyl cyclase and cAMP–>relax bronch smooth m
-
-long DOA
-tachycardia, muscle tremor, headache
-bronchodilate
Salmeterol with Fluticasone
-Beta-2 agonist with corticosteroid
-stim adenyl cyclase and cAMP–>relax bronch smooth m
-
-combination necessary in maintenance therapy
-
-maintenance bronchodilation
Beclomethasome
-corticosteroid
-inhibit inflam. response system thru gene expression
-
-topical inhalation
-generally none
-long term asthma reduction
Budenoside
-corticosteroid
-inhibit inflam. response system thru gene expression
-
-topical inhalation
-generally none
-long term asthma reduction
Fluticasome
-corticosteroid
-inhibit inflam. response system thru gene expression
-
-topical inhalation
-generally none
-long term asthma reduction
Prednisone
-corticosteroid
-inhibit inflam. response system thru gene expression
-
-oral or intravenous
- glucose metab.,Cushing’s, hypert, increased infection
-asthma
Triamcinolone
-corticosteroid
-inhibit inflam. response system thru gene expression
-
-topical inhalation
-generally none
-long term asthma reduction
Montelukast
-leukotriene modulator
-receptor antagonist of LTD4
-
-oral
-
-long-term controller of asthma
Zafirlukast
-leukotriene modulator
-receptor antagonist of LTD4
-
-oral
-
- long term controller of asthma
Zileuton
-leukotriene modulator
-inhibitor of 5-lipoxygenase inhibiting synthesis of LTB/D4
-
-oral
-liver toxicity, and inhibits some CYPs
-long term controller of asthma
Cromolyn
- degranulation inhibitor
- possible inhibit of Ca channels in Mast cell degranulation
- poorly soluble salt
- Topical
- well tolerated
- long term prophylactic maintenance of asthma
Nedocromil
- degranulation inhibitor
- possible inhibit of Ca channels in Mast cell degranulation
- poorly soluble salt
- Topical
- well tolerated
- long term prophylactic maintenance of asthma
Ipratropium
-muscarinic cholinergic antagonist - -quaternary ammonium -shorter DOA, topical inhalant -tachycardia, decreased salivation -bronchodilation and min. mucociliary clearance problems
Theophylline
- Misc. Bronchodilator
- inhibit phosphodiesterase degradation of cAMP
- methylxanthine
- oral, LongDOA
- tachycardia and CNS stimulation
- long-term maintenance of asthma
