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.
