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825 - Therapeutics 1 > Representative Drugs > Flashcards

Representative Drugs Flashcards

1
Q

Acetylcholine

A

-Muscarinic agonist

ACh is the primary transmitter of all preganglionic neurons.

  • NT in all PSNS postganglionic neurons is Acetylcholine
  • SNS postganglionic sweat glands also release ACh for thermoregulation purposes, but that’s it.
  • Included in cholinergic pharmacology

Used for intraocular miosis during surgery

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2
Q

Muscarine

A
  • Muscarinic agonist

Muscarine is an exogenous drug that binds to the muscarinic receptor.

  • Although it has no chiral carbons, it does have a fixed stereochemistry when it binds to the muscarinic receptor, and that’s what synthetic drugs try to mimic when targeting the muscarinic receptor.
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3
Q

Pilocarpine

A
  • M3 agonist

This has 2 5-membered rings, but still binds to muscarinic receptor. This stimulates the contraction of the ciliary muscle, thus increasing the outflow of aqueous humor and decreasing intraocular pressure.

This is good for patients with glaucoma, and for treating Xerostomia (dry mouth, cottonmouth) & Sjogren’s syndrome (salivary gland secretion reduced).

Use caution if patient has cardiac disease or asthma.

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4
Q

Bethanechol

A
  • Muscarinic agonist

Resembles ACh, but has less AChE hydrolyzation due to carbamate and b-methyl group.

Good for patients needing GI stimulation or treatment of urinary retention.

Use caution if patient has cardiac disease or asthma.

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5
Q

Carbachol

A
  • Muscarinic agonist

Resembles ACh, but has less AChE hydrolyzation due to carbamate.

Good for ocular surgery and glaucoma.

Use caution if patient has cardiac disease or asthma.

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6
Q

Methacoline

A
  • Muscarinic agonist

Resembles ACh, but has less AChE hydrolyzation due to methyl group.

Good to use as provocative test for hyperreactive airways

Use caution if patient has cardiac disease or asthma.

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7
Q

Edrophonium

A
  • Reversible anticholinesterase inhibitor

Edrophonium is very short acting. This has a quaternary amine and an -OH on the aromatic ring.

Used in the diagnosis of Myastenia Gravis (MG), which is an autoimmune disorder that causes muscle weakness due to the loss of skeletal muscle nicotinic receptors.

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8
Q

Neostigmine

A
  • Reversible anticholinesterase inhibitor

This has a quaterenary amine and is a carbamate.

Used for MG & reversal of the nondepolarizing neuromuscular blockage and post-up urinary retention

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9
Q

Physostigmine

A
  • Reversible anticholinesterase inhibitor

Physostigmine has CNS access due to no quaternary amine.

Used for glaucoma, Alzheimer’s disease, and as an antidote to anticholinergic overdose.

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10
Q

Pyridostigmine

A
  • Reversible anticholinesterase inhibitor

Pyridostigmine has a quaternary amine and a carbamate.

Used in treatment of MG, reversal of nondepolarizing neuromuscular blockade, and pretreatment for potential nerve gas exposure (MOA is to occupy AChE so that the nerve gas has nowhere to go).

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11
Q

Echothiophate

A
  • Irreversible anticholinesterase inhibitor

This has a quaternary amine and a S-P bond.

This was used in treatment of glaucoma because it enhances the activity of muscarinic receptors.

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12
Q

Sarin

A
  • Irreversible anticholinesterase inhibitor

This has a P-F bond.

This is a nerve gas, so it’s used as a poison.

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13
Q

Malathion

A
  • Irreversible anticholinesterase inhibitor

This has an S-P bond and kinda acts like a prodrug.

Malathion is used as an insecticide because it’s not toxic in mammals, due to it being inactivated very quickly by carboxyesterases.

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14
Q

Nicotine

A

This is an exogenous compound that binds to the nicotinic receptor (nicotinic agonist).

At low doses, this stimulates the reticular activating system and releases dopamine (addictive). At higher doses, this causes CV effects like HTN and tachycardia. At toxic doses, it can cause seizures, GI disturbance, etc.

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15
Q

Varenicline

A
  • Partial agonist of nicotinic receptor

This produces a low to moderate release of dopamine that rewards the brain, which reduces withdrawal syndromes. It also blocks the binding of nicotine and therefore blocks the positive reinforcement.

This is great for smoking cessation

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16
Q

Scopolamine

A
  • Muscarinic antagonist (3º amine)

Scopolamine resembles atropine, but is more lipophilic.

This is used to treat GI/urinary conditions, Motion sickness, and as an adjuct for Parkinsons.

This should not be used for ocular applications due to the long duration of effect.

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17
Q

Ipratropium

A
  • Muscarinic antagonist (4º amine)

Ipratropium has a quat. amine, but other than that it really mimicks atropine.

This is used for COPD and occasionally for asthma. It’s an M3 antagonist, so it blocks the ACh-mediated constriction and opens the airways.

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18
Q

Tolterodine

A
  • Muscarinic antagonist (3º amine)

Looks kinda like atropine, but has 2 aromatic rings and no ester.

This is used to treat overactive bladder.

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19
Q

Atropine

A
  • Muscarinic receptor antagonist

Has BBB access because it’s only a 3º amine.

This is used in combination with 2-PAM to treat organophosphate toxicity. This works because it blocks the muscarinic receptors so that all the excess ACh can’t keep activating them.

At different doses, atropine is used for different things: OTC cold remedy, opthalmic exams or procedures, COPD and asthma, reduce urinary frequency, anti-motion sickness & anti-parkinson’s.

Also used as a treatment to cholinergic side effects, like salivation, lacrimation, urination, and defecation (SLUD)

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20
Q

Pralidoxime (2-PAM)

A
  • AChE inhibitor antidote

This is great for pesticide or nerve gas poinsoning. The O- is a strong nucleophile that hydrolyzes the organophosphate.

This doesn’t cross the BBB, so it needs to be combined with atropine.

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21
Q

Succinylcholine

A
  • Nicotinic antagonist (neuromuscular blocking agent)

This displays a depolarizing blockade, meaning it first activates, then blocks the nicotinic receptor. It is essentially an ACh dimer.

It’s used for skeletal muscle relaxation during anesthesia and for electro-convulsant therapy.

This is bad for pts with HTN because this can raise blood pressure. Also bad for pts with hyperkalemia because it can cause cardiac arrest.

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22
Q

Tubocurine

A
  • Nicotinic antagonist (neuromuscular blocking agent)

Tubocurine has a really bulky structure, but has a few components that makes it bind to the nicotinic receptor.

This displays a non-depolarizing blockade, meaning it binds and then blocks the active site of the nicotinic receptor.

This is used for skeletal muscle relaxation during anesthesia, so it’s great for pts who need to be intubated.

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23
Q

Hexamethonium

A
  • Ganglionic nicotinic receptor antagonist

This blocks all SNS and PSNS activity. It was originally used to treat hypertension, but it causes so many adverse effects that it’s not used anymore.

Problems:
Sweat glands (SNS) - decreases perspiration
Heart rate (PSNS) - tachycardia
Other glands (PSNS) - dry mouth, decreased secretions
Eye (PSNS) - pupillary dilation and blurred vision
Blood vessels (SNS) - hypotension
Gut (PSNS) - constipation
Bladder (PSNS) - urinary retention

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24
Q

Botulinum Toxin

A
  • Blocks ACh release

This inhibits the fusion and depolarizing of the synaptic vessel, thus relaxing (paralyzing) the muscle.

Clinically, it’s used for dystonias, cerebral palsy, spasms of ocular muscles, anal fissures, and hyperhidrosis.

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25
Q

Epinephrine

A
  • α1, α2, β1 and β2 agonist

Leads to vasoconstriction (a1), cardiac stimulation (b1), and vasodilation (b2).

This is used for anaphylaxis, glaucoma, and in combination with local anesthetics.

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26
Q

Norepinephrine

A
  • α1, α2, and β1 agonist

Leads to vasoconstriction -> rise in BP (a1); Stimulates heart by increase in force and contraction (b1).

This is used as a pressor (increase BP)

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27
Q

Dopamine

A
  • D1 and β1 agonist at low doses, α1 agonist at high doses.

Leads to vasodilation in renal, mesenteric, and coronary arteries, thus increasing blood flow (D1); Cardiac stimulation (b1); @ high dose -> Vasoconstriction (a1).

Used during shock and useful for acute congestive heart failure.

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28
Q

Cocaine

A
  • Norepinephrine transporter inhibitor

Actually kind of looks like atropine. This blocks the reuptake of NE.

This can be used as a local anesthetic for nasal mucosa and vasoconstriction.

This is bad for HTN pts and has high addictive potential.

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29
Q

Methylphenidate

A
  • NET inhibitor

Blocks NE and DA reuptake transporters, thus enhancing NE and DA signaling.

Used for ADHD and narcolespy, just like amphetamine.

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30
Q

Atomoxetine

A
  • NET inhibitor

Enhances NE levels by inhibiting NET.

Used for ADHD

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31
Q

Amphetamine and methamphetamine

A
  • Indirect acting sympathomimetic

Has no -OH on the aromatic, no β-OH, but it does have an α-methyl.

This is used for ADHD, narcolepsy, and as an anorexiant.

This is potentially dangerous for those with HTN or addiction problems.

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32
Q

Ephedrine/Pseudoephedrine

A
  • Indirect acting sympathomimetics

No -OH on the aromatic. There is an α-methyl group, which protects against MAO, making this orally available.

Pseudoephedrine is used as a nasal decongestant.
Ephedrine doesn’t have any PDA approved uses.

This is bad for patient with HTN and for patients taking an MAO-inhibitor.

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33
Q

Metyrosine

A
  • Indirect adrenergic inhibitor

This inhibits Tryosine -> Dopa, thus inhibiting the formation of all neurotransmitters.

Can be use in preoperative pheochromocytoma treatment

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34
Q

Phenylephrine

A
  • α1 receptor agonist

Norepinephrine with just one -OH on the aromatic ring.

Used for mydriasis without paralysis of the ciliary muscle, to raise blood pressure, and as a nasal decongestant.

Not good if pt already has HTN.

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35
Q

Clonidine

A
  • α2 agonist

Clonidine is an imidazolidine, which lowers the pKa and gives it CNS access.

Used to treat HTN, opiate withdrawal, and ADHD.

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36
Q

Brimonidine

A
  • α2 agonist

This doesn’t look much like NE. It has 3 rings and an attached Br.

Can be used to inhibit the production and increase the outflow of aqueous humor, thus decreasing intraocular pressure.

This is great for patients with glaucoma.

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37
Q

Methyldopa

A
  • α2 agonist

This is a prodrug that when active, acts at the a2 receptors to decrease sympathetic outflow.

Used to treat hypertension, especially during pregancy.

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38
Q

Isoproterenol

A
  • Non-selective direct acting β agonist

Has a bulky group attached to the amine and a catechol.

Used to treat asthma, COPD, and as a cardiostimulant.

This shouldn’t be used if the pt has HTN, because it will increase the cardiac output.

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39
Q

Dobutamine

A
  • Mixed β1 and α1 agonist

Has a long bulky group as the R group, but doesn’t have the β-OH group. Also it’s a catechol (COMT).

One enantiomer is potent for b1, and the other enantiomer is more potent for a1. This results in a positive inotropic effect on the heart with little chronotropic effect.

This is used for acute heart failure and shock.

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40
Q

Albuterol

A
  • β2-selective agonist

Has a bulkly R group and hydroxymethyl group, which makes it selective for b2.

Causes bronchodilation, so it’s used to treat asthma and COPD.

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41
Q

Terbutaline

A
  • β2-selective agonist

Has bulky R group and resorcinol on the aromatic ring, making it b2 selective.

Used as a tocolytic, meaning it relaxes the uterus during premature labor.

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42
Q

Mirabegron

A
  • β3 agonist

Long and bulky R group and no -OH on the aromatic ring.

Used for overactive bladder.

This shouldn’t be used if the pt has HTN.

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43
Q

Phenoxybenzamine

A
  • non-selective α antagonist (irreversible)

Haloalkylamine. This results in a covalent bond, making it an irreversible inhibitor.

Used to treat pheochromacytoma and for hypertensive crisis.

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44
Q

Phentolamine

A
  • non-selective α antagonist (reversible)

Imidazoline. Competitive blocker.

Used to treat pheochromacytoma, male impotence, and for hypertensive crisis

This cannot be used for HTN because although it’s a potent vasodilator, the baroreflex causes tachycardia.

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45
Q

Prazosin

A
  • α1 antagonist

Quinazoline ring + acyl moiety.

Used to treat HTN, Reynaud’s disease, and benign prostatic hypertrophy.

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46
Q

Tamsulosin

A
  • α 1A blocker

Derivative of phenylethylamine.

This is very selective to the prostate urethra, because that area is rich in alpha1A receptors. This drug is less prone to induce hypotension (like Prazosin would).

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47
Q

Propranolol

A
  • non-selective β blocker

Aryloxypropanolamine with a tert-butyl. This is liophilic and bulky, making it selective for the β receptors.

Used for HTN, angina, cardiac arrhythmias, migraine, stage fright, thyrotoxicosis, glaucoma, and CHF.

This shouldn’t be used for pts who have asthma, because it’ll antagonist the bronchodilation effects of the β2 receptor.

Also be sure to taper the dose when D/C due to potential rebound HTN.

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48
Q

Timolol

A
  • Non-selective β antagonist

Has a thiadiazole nucleus with morpholine ring.

Used to treat glaucoma mainly, HTN, angina, and migraine.

This shouldn’t be used for pts who have asthma, because it’ll antagonist the bronchodilation effects of the β2 receptor. Also be sure to taper the dose when D/C due to potential rebound HTN.

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49
Q

Metoprolol

A
  • selective β1 antagonist

Has bulky R group and the single aromatic ring with a para group. This makes it selective to β1, and therefore it’s referred to as “cardioselective.”

Used for HTN, angina, antiarrhythmic, CHF.

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50
Q

Carvedilol

A
  • mixed adrenergic receptor antagonist (β and α1 blocker)

This is an aryloxypropylamine. The β-blocking activity prevents the reflex tachycardia that’s normally associated with α1 receptor antagonists.

Carvedilol is used for HTN and CHF.

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51
Q

Labetalol

A
  • mixed adrenergic receptor antagonist (β and α1 blocker)

This is a phenylethylamine derivative. The β-blocking activity prevents reflex tachycardia normally associated with α1 receptor antagonists.

This is used to treat HTN and hypertensive crisis.

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52
Q

Reserpine

A
  • Catecholamine depleter

This structure is aromatic and extremely bulky. It blocks VMAT, thus depleting the vesicular pool of NE (and all catecholamines).

This is used in the treatment of HTN, but not very common due to adverse effects.

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53
Q

Nadolol

A
  • Non-selective β antagonist

This is less lipophilic than propranolol.

Used for HTN, angina, and migraine.

Don’t use this in patients with kidney disease because it’s mostly excreted unchanged in the urine.

54
Q

Pindolol

A
  • Non-selective β antagonist

This has intrinsic sympathomimetic activity, making it a partial agonist.

This is used to treat HTN, angina, and migraine, and is good for patients who have severe bradycardia or little cardiac reserve, because it’s less likely to cause bradycardia & lipid abnormalities due to the partial agonist characteristic.

55
Q

Esmolol

A
  • β1 antagonist

This has the single aromatic ring with para substituent, but it has an extremely short half life of 9 minutes due to rapid hydrolysis by esterases in RBCs.

Due to the short half life, this is used for supraventricular tachycardia, atrial fibrillation/flutter, and for perioperative hypertension.

There aren’t many side effect for this due to the short half life. Also, this is incompatible with sodium bicarbonate, so make sure the pt isn’t taking sodium bicarb.

56
Q

Bretylium tosylate

A
  • Indirect adrenergic inhibitor

This is an aromatic quaternary amine. It displaces and releases NE, and prevents further release.

It is used as an antiarrhythmic, but has side effects so it’s not super common.

57
Q

Aminoglutethimide

A
  • Blocks steroid synthesis

This inhibits aromatase and P450scc, so it inhibits Cholesterol -> Pregnenolone.

This is used to block steroid production in some hormone-dependent tumors (breast, prostate).

58
Q

Ketoconazole

A
  • Blocks steroid synthesis

At higher conc., this inhibits P450scc, 17α-hydroxylase, and 11β-hydroxylase.

Used to treat hyperglucocorticoid states as seen in Cushing’s syndrome.

59
Q

Testosterone

A

17α-OH, 3-ketone

Used clinically for androgen replacement therapy in men, gynecologic disorders, as a protein anabolic agent, and for andropause.

Should not be used in infants or pregnant women because significant disturbances in sexual development may occur.

60
Q

Finasteride

A
  • 5α-reductase inhibitor; Reduces active testosterone

Resembles testosterone but has a bulky group on C17. These inhibit the conversion from testosterone -> 5α-dihydrotestosterone

This is used in treatment of benign prostatic hyperplasia, male pattern baldness, and hirsutism.

61
Q

Dutasteride

A
  • 5α-reductase inhibitor

Resembles testosterone but has a bulky group on C17 with lots of F.

Used to treat benign prostatic hyperplasia and male pattern baldness.

62
Q

Cyproterone

A
  • Steroidal androgen receptor inhibitor

Resembles testosterone but has a Cl on C6 and a ketone on C20.

Used for hirsutism in women and excessive sexual drive in men.

63
Q

Spironolactone

A
  • Steroidal androgen receptor inhibitor

Resembles testosterone, but has sulfur group on C7 and more bulky group on C17.

Used for hirsutism in women and acne.

64
Q

Flutamide

A
  • Non-steroidal androgen receptor inhibitor

Used to treat prostate cancer

65
Q

Enzalutamide

A
  • Non-steroidal androgen receptor inhibitor

Used to treat metastatic castration-resistant prostate cancer.

66
Q

Diethyl Stilbestrol

A
  • Non-steroidal estrogen

Has the two opposite -OH, which increases activity.

Used in advanced prostate cancer.

Do not use this, or any steroids, if the woman is pregnant.

67
Q

Chlorotrianisene

A
  • Non-steroidal estrogen

Prodrug, has Cl group on it.

Used for postpartum breast engorgement, menopause symptoms, and prostate cancer.

Do not use this, or any steroids, if the woman is pregnant.

68
Q

Tamoxifen

A
  • SERM (Selective Estrogen Receptor Modulator)

Prodrug (-OH gets added in vivo), selective agonist, has the amine substituted side chain that inhibits helix 12.

Used to treat/prevent breast cancer.

69
Q

Toremifene

A
  • SERM

Structurally similar to tamoxifen, but this one has a Cl.

Used to treat advanced breast cancer.

70
Q

Ospemifene

A
  • SERM

Structurally similar to Toremifene (has the Cl), but no longer has the amine substituted side chain (replaced by OH chain).

This is used to treat dyspareunia (painful sex) in post-menopausal women.

71
Q

Raloxifene

A
  • SERM

Has the two -OH groups and amine substituted group. It has estrogen and antiestrogen actions.

Prevents osteoporosis in postmenopausal women (estrogen action), but increases the risk for blood clots. It also reduces the risk for breast cancer (antiestrogen).

72
Q

Clomiphene

A
  • SERM

Has amine substituted group and Cl.

This is used to stimulate ovulation in women with irregular or no period. It does this by increasing the secretion of FSH and LH (inhibits negative feedback). A common condition that needs this is Polycystic ovary syndrome (PCOS)

73
Q

Fulvestrant

A
  • SERD (selective estrogen receptor downregulator)

Has the steroidal 4-ring structure with a long S and F substituent on carbon 7.

Used in the treatment of breast cancer, and is especially good for patients who have become resistant to tamoxifen.

74
Q

Anastrozole, Letrozole, Exemestane

A
  • Aromatase inhibitors

Anastrozole and Letrozole are non-steroidal.
Exemestane has the 4-ring structure.

Used for gynecomastia (enlargement of male breasts) and off-label for ovulation induction (reduces estrogen negative feedback).

75
Q

Levonorgestrel

A

-2nd gen Progestin

Very similar structure to norethindrone, but has an ethyl group on C13.

Used in IUDs.

76
Q

Progesterone, Norethindrone, Ethynodiol diacetate

A
  • 1st gen progestins

Norethindrone has a H which replaces the 19-methyl on progesterone, giving it more acitivity. It also has a 17-ethynyl to increase oral bioavailability.

Ethynodiol diacetate is similar to norethindrone, but has ester on C3 and on C17, thus prolonging the half-life.

These are used as oral contraceptive, hormone replacement therapy, for endometriosis, dysmenorrhea, bleeding disorders.

77
Q

Norgestimate

A
  • 2nd gen progestins

Similar to levonorgestrel, but has an ester on C17, and an N-OH group on C3. It’s a prodrug that is converted to levonogestrel in vivo.

Used as oral contraceptive, hormone replacement therapy, for endometriosis, dysmenorrhea, bleeding disorders.

78
Q

Desogestrel -> Etonogestrel

A
  • 3rd gen progestin

Desogestrel is a prodrug. When the C3 ketone gets added, it is now Etonogestrel. It is structurally analogous to levonorgestrel (but also has ketone on C11).

Desogestrel has high oral bioavailability. Etonogestrel is used in the subdermal implant or vaginal ring.

79
Q

Drospirenone

A
  • 4th gen progestin

Similar to progestin, but has C18 & C19 methyls. Also has 5 membered ring structure on C17. And triangle looking things on rings 2 & 4.

It has relatively weak progestogenic activity (only 10% of levonorgestrel), and has antimineralocorticoid activity (reduces the edema).

This is great because it negates the side effects of ethynyl estradiol in combination therapy.

80
Q

Medroxyprogesterone acetate

A
  • 1st gen progestin

It is more hydrophobic, so it’s used for depot injection.

81
Q

Ulipristal acetate (Ella)

A

-SPRM (selective progesterone receptor modulator)

This is similar to progesterone, but has especially bulky group on C11.

This is used as an emergency contraceptive and can be effective up to 5 days after unprotected sex.

This may cause nausea and abdominal pain.

82
Q

Mifepristone

A
  • Progesterone antagonist

This is similar to progesterone, but has especially bulky group on C11.

This is used in combination with misoprostol to terminate pregnancy.

83
Q

Danazol

A
  • Weak androgen, weak progestin, and antiestrogen

This is similar to progesterone, but has a 5 membered ring attached to ring 1.

This is used for endometriosis because it inhibits the surges of LH and FSH and suppresses ovarian function.

This should not be used in patients with hepatic dysfunction, or those who are pregnant/breast feeding.

84
Q

Alprostadil

A
  • Eicosanoid: PGE (dilation)

This is used for erectile dysfunction by injection or as a suppository.

85
Q

Misoprostol

A
  • Eicosanoid: PGE derivative (dilation)

Used to terminate early pregnancy with mifepristone and it prevents peptic ulcer.

86
Q

Lantanoprost

A
  • Eicosanoid: PGF (constrict)

Has a ring on one of the carbon chains

Used in opthalmology to treat glaucoma.

87
Q

Prostacyclin

A
  • Eicosanoid: PGI (inhibit aggregation)

One of the carbon chains is very ring like.

This is a powerful dilator that is used to treat pulmonary arterial hypertension by IV or inhalation.

This should not be used if the pt is taking anticoagulants because it would double the action of them.

88
Q

Salicylic acid

A
  • NSAID: Salicylates

Simple aromatic ring with -OH and -CO2H.

Used to be used as an antipyretic/antirheumatic. It reversibly inhibits COX1 and COX2.

89
Q

Aspirin

A
  • NSAID: Salicylates

Salicylic acid, but an acetyl instead of OH.

Among the usual uses of pain, fever, and inflammation, this blocks clotting, thus decreasing the risk of bleeding and reducing risk of MI.

90
Q

Salsalate

A
  • NSAID: Salicylate

Dimer of salicylic acid (prodrug)

Treats usual NSAID things (pain, fever, inflammation).
Doesn’t cause GI bleeding because it’s a prodrug!

91
Q

Diflunisal

A
  • NSAID: Salicyclate

Similar to dimer of salicylic acid, but has 2 Flourines on one ring.

This has less antipyretic acitvity than aspirin, but has a much longer half life.

92
Q

Indomethacin

A
  • NSAID: Arylacetic acid

This is one of the most potent NSAIDs in use.

This should not be used for long term use due to the side effects.

93
Q

Sulindac

A
  • NSAID: Arylacetic acid

This is a prodrug.

This has less GI side effects due to it being a prodrug.

This is good for long-term use to treat chronic inflammation.

94
Q

Etodolac

A
  • NSAID: Arylacetic acid

This is a pyranocarboxylic acid. It is somewhat selective for COX-2 so there is less GI bleeding. It is just as potent as indomethacin.

This is good for long-term use to manage osteoarthritis.

95
Q

Diclofenac

A
  • NSAID: Arylacetic acid

This looks similar to indomethacin and is just as potent. It’s somewhat selective for COX2. Most widely used NSAID in the world!!!

This inhibits both COX and lipoxygenase pathways.

This does all the NSAID function, so it’s good for pain and arthritis.

96
Q

Ibuprofen

A
  • NSAID: Arylpropionic acid

More potent than aspirin, but less potent than indomethacin. The a-methyl group enhances its activity and reduces many of its side effects.

Used for pain and inflammation.

97
Q

Naproxen

A
  • NSAID: Arylpropionic acid

More potent than ibuprofen.

This is good for long term use for treating rheumatoid arthritis and osteoarthritis

98
Q

Ketorolac

A
  • NSAID: Arylpropionic acid

This is a cyclized heteroarylpropionic acid derivative.

It is used for short-term management of moderate to severe pain and is widely accepted as an alternative to narcotic analgesics. (Bad for long term use)

99
Q

Nabumetone

A
  • NSAID: Non-carboxylates

This is a prodrug that gets converted into a carboxylic acid.

This is good for inflammation, but only has weak analgesic purposes.

100
Q

Meloxicam

A
  • NSAID: Non-carboxylates

This is as potent as indomethacin and is somewhat selective for COX-2.

This is good because it’s long acting so you only need one daily dose. This is good for arthritis.

101
Q

Celecoxib

A
  • NSAID: Selective COX-2 inhibitor

This is as potent as naproxen, has less GI side effects, and no antiplatelet activity.

This is used for osteoarthritis and rheumatoid arthritis. It’s also good for pain, inflammation, and fever.

102
Q

Acetaminophen

A

This scavenges peroxynitrite, which is required for PGH synthase activity, so this indirectly inhibits prostaglandin synthesis. However, it gets overwhelmed during inflammation.

This is good as an analgesic and antipyretic.

This has fewer adverse effects than aspirin due to less GI disturbance and it’s not associated with Reye’s syndrome. But, this is bad if pt have liver damage, because it can also cause liver damage.

103
Q

Fludrocortisone

A
  • Synthetic glucocorticoid

Has 9a-F (instead of H) in hydrocortisone), which gives it greater glucocorticoid activity, but still has strong mineralocorticoid activity.

Due to the edema caused by Na+ retention, this really can only be used in mineralocorticoid replacement therapy.

104
Q

Prednisone/Prednisolone

A
  • Synthetic glucocorticoid

Has extra double bond between C1 and C2, giving it an altered ring structure. It now has more potent GC activity and less MC activity.

Used for allergic reactions, inflammation, asthma, etc.

Bad for long term use.

105
Q

Methylprednisolone

A
  • Synthetic glucocorticoid

Prednisolone + 6a-methyl group. This has potency similar to prednisolone, but it has reduced MC activity.

Used for allergic reactions, inflammation, asthma, etc.

106
Q

Triamcinolone

A
  • Synthetic glucocorticoid

Has 9a-F and 16a-OH. GC same as prednisone & reduced MC. This has low oral bioavailability due to the extra OH.

107
Q

Dexamethasone

A
  • Synthetic glucocorticoid

This has a 16a-methyl group. This gives it increased lipophilicity, making it the strongest glucocorticosteroid.

Used for allergic reactions, inflammation, asthma, etc.

It has great oral availability because it has high intensity and is long acting.

108
Q

Betamethasone

A
  • Synthetic glucocorticoid

This is the enantiomer of dexamethasone, so it has similar properties (strongest glucocorticosteroid).

Used for allergic reactions, inflammation, asthma, etc.

109
Q

Triamcinolone acetonide

A
  • Inhaled glucocorticoid

Acetonide makes it resistant to hydrolysis, meaning it’s super hydrophobic now. It’s super potent (8x more than prednisolone).

Used for asthma.

110
Q

Beclomethasone dipropionate

A
  • Inhaled glucocorticoid

After being hydrolyzed, it is 14x more potent than dexamethasone, which is already the strongest glucocorticosteroid.

111
Q

Flunisolide

A
  • Inhaled glucocorticoid

Has acetonide and 6a-F. This undergoes extensive first-pass metabolism so there are minimal systemic effects.

This is an inhaler used for asthma.

112
Q

Budesonide

A
  • Inhaled glucocorticoid

This has 16,17-butylacetal. This undergoes extensive first-pass metabolism.

Used for asthma.

113
Q

Mometasone furoate

A
  • Inhaled corticosteroid

Has more bulky group on C17-a and a Cl attached on C21.

Used for asthma.

Not the best for topical use because even though they have high lipophilicity and binding affinity, they are not soluble (they make crystals)

114
Q

Fluticasone propionate

A
  • Inhaled corticosteroid

Has a thioester that is rapidly hydrolyzed, which is good for inhalers.

Used for asthma.

Not the best for topical use because even though they have high lipophilicity and binding affinity, they are not soluble (they make crystals)

115
Q

What are these and order the by potency:

Fluocinonide
Triamcinolone acetonide
Betamethasone valerate

A

Triamcinolone - high potency
Fluocinonide - high potency
Betamethasone valerate - medium potency

These are topical glucocorticosteroids. We want them to be really lipophilic. Acetonide or ester forms have the best potency due to high lipophilicity.

116
Q

Clobetasol propionate, halobetasol propionate, halcinonide

A

These are all topical corticosteroids with 21-choro attachment, which enhances the topical anti-inflammatory activity.

117
Q

Menthol, Camphor, Oil of Wintergreen (methyl salicylate)

A
  • Topical therapy for OA

This is a counterirritant

Cons: Because the dose is multiple times x day, there is adherence issues. Also issues with the smell of these

118
Q

Capsaicin cream

A
  • Topical therapy for OA

Cons: Adherence, takes 2-4 weeks to see results

119
Q

Diclofenac gel

A
  • Topical therapy for OA

Cons: adherence

Not good for pts who are taking a systemic NSAID

120
Q

Diclofenac suspension

A
  • Topical therapy for OA (knee only)

Cons: smell and adherence

121
Q

Acetaminophen (OA)

A

Dose - max 4g per day.

This requires a 2-4 week trial

MOA - inhibits synthesis of prostaglandins

Use this as schedules, don’t “chase the pain”

Make sure to use caution if pt has heavy EtOH intake or pre-existing liver disease.

122
Q

NSAIDs (OA)

A

If one doesn’t work, use a different NSAID.

Be cautious of adverse effects

Also be cautious of pts with CHF, NTH, renal dysfunction, and dehydration due to risk of nephrotoxicity.

Also cautious with CHF and CVD due to risk of cardiovascular AEs.

123
Q

Why use celebrex instead of other NSAIDs for OA?

A

Lower incidence of GI bleeding because it is a COX-2 inhibitor.

124
Q

What are these and why are they used for OA? NSAID + PPi (naproxen + esomeprazole); NSAID + misoprostol; NSAID + H2 antagonist

A

These are used to lessen the negative GI adverse effects that are seen from just the NSAID. These combination drugs are NSAID + gastroprotective drug.

125
Q

When would you use Tramadol for OA?

A

For breakthrough pain

126
Q

When would you use duloxetine for OA?

A

For breakthrough pain if tramadol doesn’t work. Don’t start with this though.

127
Q

What is Glucosamine/Chondroitin used for with OA?

A

These stimulate proteoglycan synthesis, so this can help the joints.

Be cautious if pt has diabetes or HTN because this can cause insulin resistance.

Tylenol & NSAIDs are the first go tos.

128
Q

When are intra-articular corticosteroid injections used? (OA)

A

Used for isolated joints, no more than ever 4-6 months.

This is used for pts that aren’t candidates for joint replacement/surgery

129
Q

When are hyaluronate injections used? (OA)

A

Used for pts who don’t tolerate other treatments or if they aren’t candidates for surgery.

This temporarily increases viscosity in the joint, but it takes 2-3 months to get max benefit.

130
Q

How long does a joint replacement last for OA?

A

10-15+ years

825 - Therapeutics 1 (6 decks)

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