Analgesics/antihistamines - opioids and histamine

What are Opioids?

noninflammatory agents that alleviate pain independently of anti-inflammatory effect, Narcotic - dulls sense of pain and induces sleep

What are Mu receptors for?

Receptor for enkephalins, endorphins (physical dependence on analgesics)

What are Kappa receptors for?

Receptor for dynorphins

what are Delta receptors for?

Receptor for enkephalins

Effects of opioid agonists?

Constipation, cough suppression, respiratory depression, pupil constriction

What is Morphine? What agonist? What does it cause?

Mu agonist, does not reach brain quick (lasts 4-5 hrs), pain and (cause mental cloud, orthostatic HTN, constipation, pupil constriction, respiratory depression) - for painful disorders and sharp stabbing pain

What does Heroin do?

Gets into brain rapidly, high abuse potential, legal in Europe

For pain

What do you use Codeine for?

Mild to moderate pain (no morphine like efficacy), used combined with aspirin or acetaminophen

What does Oxycodone do?

Schedule II drug, (no morphine like efficacy), treats pain

What is the length of Meperidine? What does it form? When is it contraindicated?

Shorter duration of action than morphine, forms toxic metabolite, contraindicated with heart issues

What is Fentanyl an agonist for? When do you use it (parenteral? Transdermal? Transmucosal?)

Mu agonist, most widely used synthetic opioid, short acting, (Parenteral = anesthesia, transdermal = chronic pain, transmucosal = preanesthetic meds before surgery)

When is tramadol used?

Weak Mu agonist, mild-moderate pain, use in chronic neuropathic pain

What is tolerance to a drug?

the diminishing effect with regular use of the same dose of a drug, requiring the user to take larger and larger doses before experiencing the drug's effect (rapid = N/V, Moderate = euphoria and analgesia, none = constipation and pupil constriction)

What is Physical dependence?

When drug admin stops = body functions abnormally causing withdrawal symptoms

What does histamine do?

Mediator in allergic reactions, tissue response to injury, gastric acid secretion, CNS neural modulation, released in antigen-antibody reaction

What does cromolyn sodium do? how long does it take? how is it taken?

Stabilizes mast cells and prevents release of contents (prevents histamine), takes 2-3 weeks, aerosol and nasal spray

Where H1 receptors located? what kind of response do they have?

Located on vascular, respiratory and GI smooth muscles (allergy response)

Non-sedating

What do H2 receptors do?

Regulates gastric acid secretion

Second generation H1 blockers

Non-sedating (newer)

First generation H1 blockers

Sedating

What is diphenhydramine used for? H1 first generation or second generation?

Allergies, first generation H1 blocker, OTC

What is dimenhydrinate used for? H1 first generation or second generation?

Motion sickness, cause muscle weakness/drowsiness (first generation H1)

What is fexofenadine used for? H1 first generation or second generation?

Allergies, cause less drowsiness, no toxic cardiac effects (second generation)

What is loratadine used for? H1 first generation or second generation?

Allergies, less sedating, once a day extended release (second generation)

What does cimetidine inhibit? should it be used?

Inhibit cytochrome P450 metabolism of other drugs, cause headaches, impotence, gynecomastia (SHOULD NOT BE USED)

What does ranitidine do? what does it contain? what does it cause?

Contained NDMA = recalled 2020 due to cancer causing agent, treats heartburn and gastric acid relief and Zollinger-Ellison syndrome

What does famotidine treat?

Treat heartburn, gastric acid relief, Zollinger-Ellison syndrome

Nalbuphine use? and agonist?

Used for moderate pain, Kappa receptor