Pharmacology 3 hard version

Mirtazapine, an atypical antidepressant, can cause sedation, increased appetite, and weight gain.

A class of antidepressants including Imipramine, Trimipramine, Nortriptyline, Doxepin, Desipramine, Amitriptyline, Clomipramine, and Protriptyline Amoxapine.

TCAs are used to treat depression, panic disorder, prevent migraines, and manage chronic pain syndromes.

Lower doses are often used to manage neuropathic pain. Meds like Amitriptyline are started at 5-10mg/day, and adjusted for tolerance and effectiveness.

Short-acting sleep medications like zaleplon, zolpidem, triazolam, and ramelteon are good choices for initial treatment.

Longer-acting sleep meds like zolpidem extended-release, eszopiclone, and temazepam are often preferred for sleep maintenance issues.

Start with lower doses, especially for those with liver issues or age-related considerations. Maximum doses should be considered. Example: eszopiclone maximum of 2mg.

Zolpidem binds to GABA receptors, specifically α1 subunit, which contributes to fewer side effects and lower risk of rebound insomnia.

Agonists for MT1 & MT2 melatonin receptors.

Restore dopamine levels in the basal ganglia, balancing them with acetylcholine.

Converted to dopamine in the brain to compensate for dopamine loss.

Prevents levodopa breakdown outside the brain, allowing more levodopa to reach the CNS.

Selegiline, rasagiline, and safinamide; used with levodopa to enhance its effects.

Diarrhea, orthostatic hypotension, nausea, anorexia, dyskinesias, hallucinations, sleep disorders, and potentially hepatic necrosis.

Acetylcholinesterase inhibitor; goal is to improve cholinergic transmission and prevent NMDA-glutamate receptor overstimulation in Alzheimer's.

Blocks NMDA receptors to prevent excess calcium levels, but has side effects similar to Alzheimer's symptoms.

Gabapentin and pregabalin are anticonvulsants used to treat neuropathic pain. They bind to calcium channels, with pregabalin having better absorption. Common side effects include dizziness, drowsiness, fatigue, and peripheral edema.

A trial of gabapentin for chronic neuropathic pain may last 2 months or longer. Pregabalin has a faster onset of action.

Carbamazepine is a first-line treatment for trigeminal neuralgia. It prevents repetitive neuronal discharge, reducing pain. It's related to tricyclic antidepressants (TCAs).

TCAs have anticholinergic and antihistaminergic effects. Their impact on serotonin and norepinephrine reuptake inhibition helps with neuropathic pain. Lower doses are used compared to depression treatment, and effects can last for 1-3 weeks.

Venlafaxine is used for both acute and chronic neuropathic pain. Duloxetine helps with painful diabetic neuropathy, fibromyalgia, chronic low back pain, and osteoarthritis.

Repeated application of capsaicin cream depletes substance P from primary afferent neurons, reducing pain. Watch for burning, stinging, or redness. Patches work faster than cream.

Ketamine reduces NMDA receptor firing. Lower doses are used than for anesthesia, and it's not used in infants under 3 months or those with schizophrenia. Higher doses may be needed with opioid-tolerant patients. Reduce baseline opioids by 25%-50% when combining with ketamine. Watch for agitation, confusion, hallucinations, and vivid imagery.

Lidocaine is used as an adjunctive or sole treatment for localized neuropathic pain.

Ethosuximide, a medication used for epilepsy, can potentially affect pregnancy. Regular monitoring of pregnancy status is essential for women of childbearing age taking this medication.

Some antiepileptic drugs, like carbamazepine, phenytoin, and topiramate, can interfere with oral contraceptives by reducing their effectiveness. This is due to their effect on liver enzymes.

Lamotrigine and levetiracetam are considered the safest antiepileptic drugs during pregnancy, as they are associated with a lower risk of birth defects compared to other options.

Phenytoin, an antiepileptic drug, can cause various side effects, including drowsiness, slurred speech, balance problems, nausea, tremors, gum overgrowth, and skin rashes.

COX-1, an enzyme found in most tissues, plays a crucial role in protecting the stomach lining against ulcers. Inhibiting COX-1 can increase the risk of gastrointestinal bleeding.

COX-2, an enzyme involved in inflammation, is highly regulated and mainly found in the brain, kidney, and bone. It is increased during inflammation and suppressed by corticosteroids.

Nociceptive pain is caused by damage to tissues, such as muscles, bones, or nerves. It is often associated with inflammation or mechanical problems.

Opioids are used for moderate to severe pain, including post-surgical pain, cancer-related pain, severe trauma, chronic pain, and breakthrough pain.

NSAIDs inhibit cyclooxygenase, preventing the conversion of arachidonic acid to prostaglandins which causes inflammation. This leads to anti-inflammatory effects, pain relief, and fever reduction.

Naloxone is an opioid antagonist that reverses opioid overdose by competitively displacing opioids from the mu-opioid receptor.

Opioids bind to mu, delta, and kappa receptors, mainly mu, reducing pain perception by inhibiting neurotransmitter release and stimulating endorphin release.

Nociceptive pain results from stimulation of pain receptors in response to tissue damage or injury.

NSAIDs are used for mild to moderate pain, strain, and sprain. They also have a dose-sparing effect when combined with opioids.

Breakthrough pain is a sudden, intense spike of pain that occurs despite ongoing pain management.

Nociceptive pain arises from tissue damage, while neuropathic pain originates from nerve damage.

Long-term opioid use can lead to tolerance, dependence, respiratory depression, and overdose. These risks are important to discuss with patients.

Patches deliver medication directly to the painful area, providing localized relief without affecting the whole body.

Drugs like finasteride and dutasteride can cause decreased libido, impotence, breast enlargement (gynecomastia), and low blood pressure when standing up (orthostatic hypotension).

These drugs act like a temporary chemical castration, disrupting the function of the testes or ovaries.

Raloxifene helps prevent osteoporosis, particularly in postmenopausal women.

Estradiol is the best form of estrogen when taken orally because it undergoes first-pass metabolism.

Mifepristone blocks progesterone, which is crucial for maintaining pregnancy, thereby leading to pregnancy termination.

Intrauterine devices (IUDs), both hormonal and non-hormonal, are safe and effective for breastfeeding mothers. Avoid contraceptives containing estrogen during early postpartum as it can affect milk supply.