Drugs up until Midterm #1 Flashcards
Capsaicin
It is used as a topical pain reliever that activates the TRPV1 directly and indirectly to make them less sensitive.
Metoprolol
Selective beta-1 blocker. Uses of β blockers include treatment of hypertension, angina, open- angle glaucoma.
Fluoxetine
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.
Physostigmine
Cholinesterase inhibitor. Short duration of action, used for glaucoma, antidote for atropine
Doxepin
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.
Amytryptiline
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.
Desipramine
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.
Topiramate
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.
Bupropion
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.
Diflusinal
“Other NSAID agent.” Diflunisal - Related to salicylates- supposed to be good for bone pain
Lyrica
Anticonvulsant used for neuropathic pain
Amphetamine
Helps dopamine be released. Adderall is an example, used to treat ADHD. It is a stimulant.
Ketoprofen
Ibuprofen-like. Ketoprofen is same properties, but more potent. Remember that NSAIDS negate the effects of anti-hypertension medications.
Guanfacine
Alpha-2 receptor agonist, helps treat hypertension and ADHD
Clonidine
Alpha-2 receptor agonist, helps treat hypertension and ADHD.
Phenytoin
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.
Lamotrigene
Anti-epileptic drugs used for Bipolar Disorder
Dopamine
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))
Nortryptiline
First-line drug treatment (3 of them, along with Gabapentin, Duloxetine, and they are all FDA approved) to manage neuropathic pain like Trigeminal neuralgia.
Cevimeline
Cholinergic agonist used to treat xerostomia in Sjogren’s Syndrome
Meperidine
“Other” opioid narcotics, for moderate pain.
Terbutaline
Beta-2 agonist
Buprenorphine
“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)
Botulinum toxin
It prevents the release of ACh. It relaxes intraocular muscles, treats muscle dystonia (spasms), removes wrinkles.
Carbamezepine
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.
Modafinil
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.
Beta-endorphins
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.
Succinylcholine
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.
Entacapone
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.
Naloxone
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
Prazosin
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.
Isoproterenol
Beta-1 and Beta-2 receptor agonist
Ephedrine
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)
Lithium Carbonate
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.
Pentazocine
“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.
Pramipexole
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.
Naproxen
Ibuprofen-like. Naproxen is longer-lasting and slower-acting (Aleve).
Quetiapine
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.
Atropine
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.
Celecoxib
Celebrex. Cox-2 selective antagonist. • Prescription only • Same analgesia as ibuprofen • Lacks GI and anti-clotting action • Warning about cardiovascular side effects
Sertraline
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.
D-tubocurarine
Nicotinic (muscle) antagonist. It is non-depolarizing and competitive. It competes with ACh at nicotinic receptors.
Cocaine
Blocks the reuptake of dopamine
Bethanechol
It is a muscarinic receptor agonist. Specifically, is a cholinesterase inhibitor.
Methadone
“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)
Ethosuximide
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.
Atenolol
Selective beta-1 blocker. Uses of β blockers include treatment of hypertension, angina, open- angle glaucoma.
Phenelzine
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
Thioridizine
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
Salicylates
They are non-selective COX-1 and COX-2 inhibitors, ibuprofen-like, so they are NSAIDS.
Dynorphins
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.
Fenoldapam
D1 receptor agonist, along with dopamine
L-dopa + Carbidopa
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.
Benztropine
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.
Propranolol
Beta-1 and Beta-2 receptor antagonist (beta blocker)
Olanzepine
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.
Duloxetine
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).
Venlaxafine
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).
Sarin
Cholinesterase inhibitor. Irreversible; long duration of action, nerve gas
Endocannabinoids
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.
Methylphenidate
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.
Phenylephrine
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.
Meloxicam
“Other NSAID agent.” Meloxicam - preferentially inhibits Cox-2 over Cox-1/ means less GI problems
Chlorpromazine
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
Barbiturates
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.
Phentolamine
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.
Phenobarbital
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.
Pilocarpine
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.
Selegiline
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
Lorazepam
Hypnotic benzodiazepine drug used to treat anxiety disorder
Albuterol
Beta-2 agonist
Acetaminophen
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.
Indomethacin
“Other” NSAID agent. Indomethacin - potent non-selective NSAID/ due to side effects not a common analgesic
Prednisone
Drug that treats Multiple Sclerosis. Bladder dysfunctions, bowel dysfunction, depression, fatigue, pain, tremors.
Diazepam
Sedative benzodiazipene drug used to treat anxiety disorder.
Enkephalins
Act on Delta and Mu receptors. 5 amino acids long. Made up of Methionine and Leucine.
Terazosin
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.
Tramadol
(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 pain like Trigeminal neuralgia.
Donepezil
Cholinesterase inhibitor. Used to treat Alzheimer’s.
Valproic Acid
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 increased 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.
Gabapentin
Anticonvulsant used for neuropathic pain
Trihexyphenidyl
Used for Parkinson’s Disease. Anticholinergic medication. Everything almost identical to Benztropine.
Clozapine
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.
Triazolam
Hypnotic benzodiazepine drug used to treat anxiety disorder
Scopalamine
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.
Haloperidol
It is a butyrophenone that is used to treat Psychotic disorders. High extrapyramidal side effects, lacks anticholinergic action
Phenoxybenzamine
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.
Alprazolam
Sedative benzodiazipene drug used to treat anxiety disorder.
Mecamylaline
Nicotinic (neuronal) antagonist
