Drugs up until Midterm #1

Question 1

Capsaicin

Answer 1

It is used as a topical pain reliever that activates the TRPV1 directly and indirectly to make them less sensitive.

Question 2

Metoprolol

Answer 2

Selective beta-1 blocker. Uses of β blockers include treatment of hypertension, angina, open- angle glaucoma.

Question 3

Fluoxetine

Answer 3

SSRI. They are popular but can give GI upset, sexual dysfunction, and depression in adolescents. They have no anti-cholinergic activity, so you don’t get dry mouth.

Question 4

Physostigmine

Answer 4

Cholinesterase inhibitor. Short duration of action, used for glaucoma, antidote for atropine

Question 5

Doxepin

Answer 5

Tri-cyclic anti-depressant. Have long half-life, single daily lose, they block the uptake of NE and varying affinity for 5HT transporters. They give dry mouth pretty bad, H1 blockade (H1 blockers are decongestants, used for reactions to allergies, look like traditional anti-histamine drugs, H2 blockers are used to treat GI problems, diminishing gastric secretions), some orthostatic hypertension, withdrawal with abrupt discontinuation and subsequent diarrhea because you are taking away anticholinergic effect.

Question 6

Amytryptiline

Answer 6

Tri-cyclic anti-depressant. Have long half-life, single daily lose, they block the uptake of NE and varying affinity for 5HT transporters. They give dry mouth pretty bad, H1 blockade (H1 blockers are decongestants, used for reactions to allergies, look like traditional anti-histamine drugs, H2 blockers are used to treat GI problems, diminishing gastric secretions), some orthostatic hypertension, withdrawal with abrupt discontinuation and subsequent diarrhea because you are taking away anticholinergic effect.

Question 7

Desipramine

Answer 7

Tri-cyclic anti-depressant. Have long half-life, single daily lose, they block the uptake of NE and varying affinity for 5HT transporters. They give dry mouth pretty bad, H1 blockade (H1 blockers are decongestants, used for reactions to allergies, look like traditional anti-histamine drugs, H2 blockers are used to treat GI problems, diminishing gastric secretions), some orthostatic hypertension, withdrawal with abrupt discontinuation and subsequent diarrhea because you are taking away anticholinergic effect.

Question 8

Topiramate

Answer 8

Used for all Partial seizures as well as Tonic-Clonic and Lennox-Gastaut syndrome seizures. This drug is unique because it is the only one that causes weight loss. Decreases word-finding ability as well. One of its side effects is that it metabolizes estrogen which will lower the efficacy of birth control. It’s MOA is that it blocks repetitive firing of Na+ channels, inhibits Ca+ channels, inhibits AMPA/Kainate receptors, and potentiates GABA currents. Know that this drug is broad spectrum and causes weight loss.

Question 9

Bupropion

Answer 9

It is used to treat anxiety disorders, and it is a non-sedating sedative, not a depressant, but still has anxiolytic activity. We use it for everyday stress and anxiety. Usually for short-term use. Not very addicting, can interact with MAO inhibitors or anti-seizure medicines.

Question 10

Diflusinal

Answer 10

“Other NSAID agent.” Diflunisal - Related to salicylates- supposed to be good for bone pain

Question 11

Lyrica

Answer 11

Anticonvulsant used for neuropathic pain

Question 12

Amphetamine

Answer 12

Helps dopamine be released. Adderall is an example, used to treat ADHD. It is a stimulant.

Question 13

Ketoprofen

Answer 13

Ibuprofen-like. Ketoprofen is same properties, but more potent. Remember that NSAIDS negate the effects of anti-hypertension medications.

Question 14

Guanfacine

Answer 14

Alpha-2 receptor agonist, helps treat hypertension and ADHD

Question 15

Clonidine

Answer 15

Alpha-2 receptor agonist, helps treat hypertension and ADHD.

Question 16

Phenytoin

Answer 16

Used for all Partial seizures as well as Tonic-Clonic seizures. It masculinizes (hirsuitism) and causes severe gingival hyperplasia, osteopenia, anemia, acne. This drug is special because it has zero-order kinetics at high doses. Most drugs have first-order kinetics. So with this, as you give Phenytoin to patients, it overcomes the metabolize enzymes in the liver, so with even the smallest increase in dose, you get an upshoot increase and can become highly toxic. You have to constantly monitor the levels in your patient. It’s MOA is that it blocks sustained high frequency of action potentials by blocking Na+ channels during repetitive firing.

Question 17

Lamotrigene

Answer 17

Anti-epileptic drugs used for Bipolar Disorder

Question 18

Dopamine

Answer 18

The adminestering of Dopamine itself is used to treat shock and heart failure (at high doses, increased BP and TPR (α1); increased HR (β1); increased organ perfusion (D1))

Question 19

Nortryptiline

Answer 19

First-line drug treatment (3 of them, along with Gabapentin, Duloxetine, and they are all FDA approved) to manage neuropathic pain like Trigeminal neuralgia.

Question 20

Cevimeline

Answer 20

Cholinergic agonist used to treat xerostomia in Sjogren’s Syndrome

Question 21

Meperidine

Answer 21

“Other” opioid narcotics, for moderate pain.

Question 22

Terbutaline

Answer 22

Beta-2 agonist

Question 23

Buprenorphine

Answer 23

“Other opioid narcotic.” (As they go to higher doses it turns into an antagonist, shuts everything off, and kicks them into withdrawals, so harder to get addicted to, similar to two above)

Question 24

Botulinum toxin

Answer 24

It prevents the release of ACh. It relaxes intraocular muscles, treats muscle dystonia (spasms), removes wrinkles.

Question 25

Carbamezepine

Answer 25

**Used for all Partial seizures as well as Tonic-Clonic seizures**. Although rare, **Steven-Johnsons Syndrome** is a side effect. This drug may also activate spike-wave seizures. It is also associated with toxic levels when patients drink **grapefruit juice**. It is a great drug for epilepsy but the potential for a drug-to-drug interaction is high. It's MOA is it **blocks Na+ channels to inhibit repetitive firing from neurons.** Also used for **Bipolar Disorder.**

Question 26

Modafinil

Answer 26

It is a minor stimulant, or non-stimulant, to treat ADHD, called the "smart drug." Has few side effects, biggest complaint is that it alters sleep patterns, and it is also used for narcolepsy.

Question 27

Beta-endorphins

Answer 27

Endogenous peptides. **Act on Delta and Mu receptors. 91 amino acids long**. -You can’t give a Beta-endorphin therapeutically, it would be proteased too quickly, but we have drugs that have opioid agonist properties that have a number of naturally occurring narcotics that have selective activities that act on mu or delta receptors.

Question 28

Succinylcholine

Answer 28

It is a **Nicotinic (muscular) antagonist**. It is **depolarizing and non-competitive**, it depolarizes/desensitizes the neuromuscular endplate; it opens the NIC channels and keeps these "open" such that the neuron is depolarized and unresponsive to another ACh challenge.

Question 29

Entacapone

Answer 29

**Used for Parkinson's Disease. It inhibits COMT, Catecholamine methyl transferase**, which metabolizes like MAO does. So works similar to Selegiline, in the sense that they are both inhibiting metabolizing agents.

Question 30

Naloxone

Answer 30

**Mu antagonist, used to treat opioid narcotic overdoses** - naloxone (Narcan). Although it may precipitate withdrawals, and it will block the endorphins (endogenous opioid systems), and if you take these alone, you will get anxiety, stress, or hypersensitivity to pain

Question 31

Prazosin

Answer 31

Alpha-1 antagonist, used to treat hypertension. It helps block vasoconstriction so essentially cause vasodilation and are used to treat hypertension as well as **benign prostatic hypertrophy** (Tamsulosin - flomax). The side effects here are also **Orthostatic hypertension and nasal stuffiness.**

Question 32

Isoproterenol

Answer 32

Beta-1 and Beta-2 receptor agonist

Question 33

Ephedrine

Answer 33

It releases NE, also some direct action on α and β receptors. Used for decongestion and dietary supplements. Side effects: increase HR, vasoconstriction, dilate airways, stimulant (if penetrates CNS)

Question 34

Lithium Carbonate

Answer 34

**Used for Bipolar Disorder.** Slow onset, likely works by **altering 2nd messenger systems** such as those involving adenylyl cyclase and G proteins, often combined with anti-depressants, still among the most potent mood stabilizers, has many side effects, **requires monitoring blood levels (narrow therapeutic window), tremors are common, kidney damage, weight gain, edema, high rate of compliance problems.**

Question 35

Pentazocine

Answer 35

"Other" opioid narcotic. It is unique because of its interaction with the **kappa receptor**, so makes it less likely that people will abuse this, it has a mixed agonist/antagonist effect.

Question 36

Pramipexole

Answer 36

This is a **dopamine agonist, a D2 agonist**, which bypasses the depleted neurons int he substantia nigra and provides long-lasting direct stimulation of dopamine receptors. Side effects include orthostatic hypertension, nausea, vomiting, confusion. **Used to treat Parkinson's Disease.**

Question 37

Naproxen

Answer 37

Ibuprofen-like. Naproxen is longer-lasting and slower-acting (Aleve).

Question 38

Quetiapine

Answer 38

**Atypical anti-psychotic drug. Besides D2 antagonism, these typically are also good 5HT2A antagonists. Little extrapyramidal side effects. Most effective against the 􏰂negative􏰄 symptoms in some forms of schizophrenia.**

Question 39

Atropine

Answer 39

**Muscarinic receptor antagonist**. **Sarin is nerve gas**, an acetylcholinesterase inhibitor, so it allows ACh to accumulate at the cleft and interact with cholinergic receptors to cause too much stimulation. You get a very slow heart rate, diarrhea, cramping, gland secretions, twitching, suffocation, blurred vision, sweating. **Soldiers carry around Atropine** as a nerve gas antidote, which will block muscarinic receptors to stop all these side effects. Atropine was originally derived from this plant on the left. And blocking these receptors would cause pupils to dilate I think. **Also helps with Parkinson's disease, motion sickness, COPD. But causes dry mouth, constipation, blurred vision, sedation, urinary retention.**

Question 40

Celecoxib

Answer 40

**Celebrex.** **Cox-2 selective antagonist.** • Prescription only • Same analgesia as ibuprofen • Lacks GI and anti-clotting action • Warning about **cardiovascular side effects**

Question 41

Sertraline

Answer 41

**SSRI**. They are popular but can give GI upset, sexual dysfunction, and depression in adolescents. **They have no anti-cholinergic activity, so you don't get dry mouth.**

Question 42

D-tubocurarine

Answer 42

**Nicotinic (muscle) antagonist.** It is **non-depolarizing and competitive**. It competes with ACh at nicotinic receptors.

Question 43

Cocaine

Answer 43

Blocks the reuptake of dopamine

Question 44

Bethanechol

Answer 44

It is a **muscarinic receptor agonist**. Specifically, is a cholinesterase inhibitor.

Question 45

Methadone

Answer 45

"Other" opioid narcotic. (If an opioid addict is going to methadone clinics, then chart that and know that you don’t need to give them more pain coverage, also used to treat opioid addiction)

Question 46

Ethosuximide

Answer 46

Used for **uncomplicated absence seizures**. Has a very narrow clinical spectrum. It's MOA is it reduces T-type Ca+ channel currents in thalamic pacemaker neurons to quiet rhythmic discharges.

Question 47

Atenolol

Answer 47

**Selective beta-1 blocker**. Uses of β blockers include treatment of hypertension, angina, open- angle glaucoma.

Question 48

Phenelzine

Answer 48

MAO A/MAO B inhibitor. They block the metabolizing enzyme for monoamines (serotonin, dopamine, epinephrine, NE), so they increase these neurotransmitters. Side effects include altered autonomic system activity, orthostatic hypertension, weight gain, may interact with foods that have **tyramine**, people have died from eating these foods and taking an MAOI inhibitor, remember these will enhance the nervous system, so when we provide local anesthetic with epinephrine, it could cause cardiovascular problems

Question 49

Thioridizine

Answer 49

**Phenothiazine, anti-psychotic drug.** Least expensive, older, more sedation and weight gain, **less extrapyramidal side effects, antiemetic action.** Anticholinergics mask the effects of tardive dyskinesias but the damage is still being done. Anticholinergics are also used to treat Parkinson’s Disease

Question 50

Salicylates

Answer 50

They are non-selective COX-1 and COX-2 inhibitors, ibuprofen-like, so they are NSAIDS.

Question 51

Dynorphins

Answer 51

Endogenous peptides. **Act on Kappa receptors.** **17 amino acids long**. There are A and B Dynorphins, they are inhibitory, they tend to block a lot of the typical reward functions. The kappa receptors are antagonistic to mew and delta, but they still have analgesic properties.

Question 52

Fenoldapam

Answer 52

D1 receptor agonist, along with dopamine

Question 53

L-dopa + Carbidopa

Answer 53

**Used for Parkinson's Disease**. L-dopa gets across blood-brain barrier much better than dopamine, and Carbidopa blocks the metabolism of L-dopa and dopamine so it can last longer. Some drugs are used in combination with carbidopa-levodopa to either inhibit dopamine breakdown by the body or to improve the effectiveness of carbidopa-levodopa. Azilect inhibits dopamine breakdown while Entacapone improves the effect of Carbidopa-levodopa by inhibiting COMT, Catecholamine Methyl Transferase, which metabolizes neurotransmitters like MAO does.

Question 54

Benztropine

Answer 54

Used for **Parkinson's Disease**. This is an **anticholinergic medication** that helps with tremors, and is effective because it counteracts the cholinergic sensitivity that arises in response to dopamine depletion. It helps dry sialorrhea from PD patients as well. It can give you confusion, blurred vision, urinary retention.

Question 55

Propranolol

Answer 55

Beta-1 and Beta-2 receptor antagonist (beta blocker)

Question 56

Olanzepine

Answer 56

**Atypical anti-psychotic drug. Besides D2 antagonism, these typically are also good 5HT2A antagonists. Little extrapyramidal side effects. Most effective against the 􏰂negative􏰄 symptoms in some forms of schizophrenia.**

Question 57

Duloxetine

Answer 57

NE or mixed transport blocker drug. They have no anti-cholinergic properties, so no dry mouth, unlike Tri-cyclics, have more CVS side effects due to increased NE/sympathetic activity, and are moderately a CNS stimulant (insomnia, anxiety).

Question 58

Venlaxafine

Answer 58

**NE or mixed transport blocker drug**. They have no anti-cholinergic properties, so no dry mouth, unlike Tri-cyclics, have more CVS side effects due to increased NE/sympathetic activity, and are moderately a CNS stimulant (insomnia, anxiety).

Question 59

Sarin

Answer 59

**Cholinesterase inhibitor**. **Irreversible; long duration of action, nerve gas**

Question 60

Endocannabinoids

Answer 60

**Anandamide** is the main endocannabinoid neurotransmitter, and it binds to **CB1 cannabinoid receptors**, and by doing so, causes **dopamine release**. Endocannabinoids are main ingredient in **marijuana.**

Question 61

Methylphenidate

Answer 61

**Indirect adrenergic agent**, similar to amphetamine, cocaine, SNRI's and TCA's. This drug **blocks DA reuptake**. It is **Ritalin**, is used for ADHD, it is a stimulant.

Question 62

Phenylephrine

Answer 62

**Alpha-1 receptor agonist** and it causes vasoconstriction to sinus vessels in order to act as a decongestant, helps with mydriasis for eye exams. Also causes a **decreased heart rate** from baroreceptor reflex essentially.

Question 63

Meloxicam

Answer 63

"Other NSAID agent." Meloxicam - preferentially inhibits Cox-2 over Cox-1/ means less GI problems

Question 64

Chlorpromazine

Answer 64

**Phenothiazine, anti-psychotic drug**. Least expensive, older, more sedation and weight gain, **less extrapyramidal side effects, antiemetic action**. Anticholinergics mask the effects of tardive dyskinesias but the damage is still being done. Anticholinergics are also used to treat Parkinson’s Disease

Question 65

Barbiturates

Answer 65

They **enhance GABA**, has **short-acting for anesthesia induction (Pentobarbital), and long-term for seizures (Phenobarbital)**. This one is a major depressor of respiration and tolerance (careful with the airway). Not frequently used, narrow margin of safety, major interactions with liver.

Question 66

Phentolamine

Answer 66

**Non-selective alpha antagonist.** Treatment of pheochromocytoma, hypertensive emergencies. Helps you get decreased TPR through blocking alpha-1 and thus decreased BP, and an increased HR through baroreceptor response to decreased BP. Major side effects are **orthostatic hypertension** and **nasal stuffiness**.

Question 67

Phenobarbital

Answer 67

Used for **all Partial seizures as well as Tonic-Clonic seizures**. Has **long-term cognitive memory and behavioral side effects**. This drug is also the **BIG TIME INDUCER**, interact with almost every drug out there. Can precipitate spike-wave seizures in patients with absence seizures. Used mainly because of low cost and broad spectrum but not great option because of side effects.

Question 68

Pilocarpine

Answer 68

**Muscarinic receptor agonist**. Used for **radiation therapy xerostomia, glaucoma, myasthenia gravis**. It acts on muscarinic receptors on iris sphincter muscle, causing the muscle to contract - resulting in pupil contraction (miosis). Pilocarpine also acts on the ciliary muscle and causes it to contract. When the ciliary muscle contracts, it opens the trabecular meshwork through increased tension. This action facilitates aqueous humor leaving the eye to decrease intraocular pressure.

Question 69

Selegiline

Answer 69

This is used for Parkinson's Disease. This is an **MAO inhibitor**, blocking **monoamine oxidase B** from metabolizing dopamine in the brain, so prolonging the effects of levodopa. Side effects include cardiac dysrhythmias. They block the metabolizing enzyme for monoamines (serotonin, dopamine, epinephrine, NE), so they increase these neurotransmitters. Side effects include altered autonomic system activity, orthostatic hypertension, weight gain, may interact with foods that have tyra mine, people have died from eating these foods and taking an MAOI inhibitor, remember these will enhance the nervous system, so when we provide local anesthetic with epinephrine, it could cause cardiovascular problems

Question 70

Lorazepam

Answer 70

Hypnotic benzodiazepine drug used to treat anxiety disorder

Question 71

Albuterol

Answer 71

Beta-2 agonist

Question 72

Acetaminophen

Answer 72

**Tylenol.** It is a Non-NSAID, Non-COX 1 or 2 inhibitor—perhaps blocks a COX 3 and/or works on 5HT. It is **non-anti-inflammatory**, has good anti-pyretic and some good analgesia. So does not help with inflammation, but can help with pain caused by inflammation.

Question 73

Indomethacin

Answer 73

"Other" NSAID agent. Indomethacin - potent non-selective NSAID/ due to side effects not a common analgesic

Question 74

Prednisone

Answer 74

Drug that treats Multiple Sclerosis. Bladder dysfunctions, bowel dysfunction, depression, fatigue, pain, tremors.

Question 75

Diazepam

Answer 75

Sedative benzodiazipene drug used to treat anxiety disorder.

Question 76

Enkephalins

Answer 76

Act on **Delta and Mu receptors**. **5 amino acids long**. Made up of **Methionine and Leucine**.

Question 77

Terazosin

Answer 77

Alpha-1 antagonist, used to treat hypertension. It helps block vasoconstriction so essentially cause vasodilation and are used to treat hypertension as well as **benign prostatic hypertrophy** (Tamsulosin - flomax). The side effects here are also o**rthostatic hypertension and nasal stuffiness.**

Question 78

Tramadol

Answer 78

(Ultram). It is a schedule 4 drug. Low drug abuse potential, but some minor opioid action. Works at brain level. **Is the "next-line" of drug treatment for neuropathic pai**n like Trigeminal neuralgia.

Question 79

Donepezil

Answer 79

**Cholinesterase inhibitor. Used to treat Alzheimer's.**

Question 80

Valproic Acid

Answer 80

**Used for all Partial seizures as well as uncomplicated absence seizures, atypical absence seizures, primary tonic-clonic seizures, and myoclonic epilepsy**. Very broad spectrum similar to Topiramate. Associated with weight gain however. As well as **Reye-like syndrome and hepatic failure.** It is strictly contraindicated with people who have liver problems. It also has an i**ncreased risk of spina bifida, category D pregnancy risk**. It's MOA is it blocks Na+ channels, reduces NMDA currents, and increases GABA at high doses. Also used for **Bipolar Disorder.**

Question 81

Gabapentin

Answer 81

Anticonvulsant used for neuropathic pain

Question 82

Trihexyphenidyl

Answer 82

**Used for Parkinson's Disease. Anticholinergic medication. Everything almost identical to Benztropine.**

Question 83

Clozapine

Answer 83

**Atypical anti-psychotic drug. Can cause serious agranulocytosis. Besides D2 antagonism, these typically are also good 5HT2A antagonists. Little extrapyramidal side effects. Most effective against the 􏰂negative􏰄 symptoms in some forms of schizophrenia.**

Question 84

Triazolam

Answer 84

Hypnotic benzodiazepine drug used to treat anxiety disorder

Question 85

Scopalamine

Answer 85

**Muscarinic Receptor Antagonist.** Along with Atropine, **Also helps with Parkinson's disease, motion sickness, COPD. But causes dry mouth, constipation, blurred vision, sedation, urinary retention.**

Question 86

Haloperidol

Answer 86

It is a **butyrophenone that is used to treat Psychotic disorders.** **High extrapyramidal side effects, lacks anticholinergic action**

Question 87

Phenoxybenzamine

Answer 87

**Non-selective alpha antagonist.** Treatment of pheochromocytoma, hypertensive emergencies. Helps you get decreased TPR through blocking alpha-1 and thus decreased BP, and an increased HR through baroreceptor response to decreased BP. Major side effects are **orthostatic hypertension** and **nasal stuffiness**.

Question 88

Alprazolam

Answer 88

Sedative benzodiazipene drug used to treat anxiety disorder.

Question 89

Mecamylaline

Answer 89

Nicotinic (neuronal) antagonist