Opioid agonists, mixed agonist-antagonists and partial agonists
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Opioid agonists, mixed agonist-antagonists and partial agonists
Prerequisite basic sciences
Abdominal pain
Anatomy of the abdominal viscera: Esophagus and stomach
Anatomy of the abdominal viscera: Innervation of the abdominal viscera
Anatomy of the abdominal viscera: Kidneys, ureters and suprarenal glands
Anatomy of the abdominal viscera: Large intestine
Anatomy of the abdominal viscera: Liver, biliary ducts and gallbladder
Anatomy of the abdominal viscera: Pancreas and spleen
Anatomy of the abdominal viscera: Small intestine
Anatomy of the female reproductive organs of the pelvis
Anatomy of the gastrointestinal organs of the pelvis and perineum
Anatomy of the male reproductive organs of the pelvis
Anatomy of the peritoneum and peritoneal cavity
Anatomy of the urinary organs of the pelvis
Anatomy of the vessels of the posterior abdominal wall
Anatomy clinical correlates: Female pelvis and perineum
Anatomy clinical correlates: Male pelvis and perineum
Anatomy clinical correlates: Other abdominal organs
Anatomy clinical correlates: Peritoneum and diaphragm
Anatomy clinical correlates: Viscera of the gastrointestinal tract
Bile secretion and enterohepatic circulation
Gastrointestinal system anatomy and physiology
Liver anatomy and physiology
Pancreatic secretion
Appendicitis: Pathology review
Diverticular disease: Pathology review
Gallbladder disorders: Pathology review
GERD, peptic ulcers, gastritis, and stomach cancer: Pathology review
Pancreatitis: Pathology review
Endocrine diseases
Anatomy of the abdominal viscera: Kidneys, ureters and suprarenal glands
Anatomy of the thyroid and parathyroid glands
Anatomy clinical correlates: Vessels, nerves and lymphatics of the neck
Anatomy clinical correlates: Viscera of the neck
Adrenal gland histology
Thyroid and parathyroid gland histology
Calcitonin
Cortisol
Endocrine system anatomy and physiology
Estrogen and progesterone
Parathyroid hormone
Phosphate, calcium and magnesium homeostasis
Synthesis of adrenocortical hormones
Testosterone
Thyroid hormones
Vitamin D
Adrenal insufficiency: Pathology review
Adrenal masses: Pathology review
Cushing syndrome and Cushing disease: Pathology review
Hyperthyroidism: Pathology review
Hypothyroidism: Pathology review
Multiple endocrine neoplasia: Pathology review
Neuroendocrine tumors of the gastrointestinal system: Pathology review
Parathyroid disorders and calcium imbalance: Pathology review
Thyroid nodules and thyroid cancer: Pathology review
Fluids and electrolytes
Introduction to the lymphatic system
Body fluid compartments
Microcirculation and Starling forces
Movement of water between body compartments
Osmoregulation
Phosphate, calcium and magnesium homeostasis
Potassium homeostasis
Renin-angiotensin-aldosterone system
Sodium homeostasis
Cirrhosis: Pathology review
Deep vein thrombosis and pulmonary embolism: Pathology review
Diabetes insipidus and SIADH: Pathology review
Electrolyte disturbances: Pathology review
Heart failure: Pathology review
Hypothyroidism: Pathology review
Nephrotic syndromes: Pathology review
Parathyroid disorders and calcium imbalance: Pathology review
Renal failure: Pathology review
Gastrointestinal hemorrhage
Anatomy of the abdominal viscera: Blood supply of the foregut, midgut and hindgut
Anatomy of the abdominal viscera: Esophagus and stomach
Anatomy of the abdominal viscera: Large intestine
Anatomy of the abdominal viscera: Small intestine
Anatomy of the gastrointestinal organs of the pelvis and perineum
Anatomy clinical correlates: Viscera of the gastrointestinal tract
Enteric nervous system
Esophageal motility
Gastric motility
Gastrointestinal system anatomy and physiology
Gastrointestinal bleeding: Pathology review
Intra-abdominal and retroperitoneal masses
Anatomy of the abdominal viscera: Kidneys, ureters and suprarenal glands
Anatomy of the abdominal viscera: Liver, biliary ducts and gallbladder
Anatomy of the abdominal viscera: Pancreas and spleen
Anatomy of the peritoneum and peritoneal cavity
Anatomy clinical correlates: Other abdominal organs
Anatomy clinical correlates: Peritoneum and diaphragm
Neuroendocrine tumors of the gastrointestinal system: Pathology review
Pancreatitis: Pathology review
Viral hepatitis: Pathology review
Jaundice
Anatomy of the abdominal viscera: Liver, biliary ducts and gallbladder
Anatomy of the abdominal viscera: Pancreas and spleen
Anatomy clinical correlates: Other abdominal organs
Gallbladder histology
Liver histology
Bile secretion and enterohepatic circulation
Liver anatomy and physiology
Pancreatic secretion
Jaundice: Pathology review
Non-cardiac chest pain and shortness of breath
Anatomy of the abdominal viscera: Blood supply of the foregut, midgut and hindgut
Anatomy of the abdominal viscera: Esophagus and stomach
Anatomy of the abdominal viscera: Innervation of the abdominal viscera
Anatomy of the diaphragm
Anatomy of the inferior mediastinum
Anatomy of the larynx and trachea
Anatomy of the lungs and tracheobronchial tree
Anatomy of the pharynx and esophagus
Anatomy of the pleura
Anatomy of the superior mediastinum
Bones and joints of the thoracic wall
Muscles of the thoracic wall
Vessels and nerves of the thoracic wall
Anatomy clinical correlates: Mediastinum
Anatomy clinical correlates: Pleura and lungs
Anatomy clinical correlates: Thoracic wall
Bronchioles and alveoli histology
Esophagus histology
Trachea and bronchi histology
Alveolar surface tension and surfactant
Anatomic and physiologic dead space
Breathing cycle and regulation
Diffusion-limited and perfusion-limited gas exchange
Gas exchange in the lungs, blood and tissues
Lung volumes and capacities
Pulmonary shunts
Regulation of pulmonary blood flow
Respiratory system anatomy and physiology
Ventilation
Ventilation-perfusion ratios and V/Q mismatch
Zones of pulmonary blood flow
Chewing and swallowing
Enteric nervous system
Esophageal motility
Gastric motility
Gastrointestinal system anatomy and physiology
Aortic dissections and aneurysms: Pathology review
Deep vein thrombosis and pulmonary embolism: Pathology review
Pleural effusion, pneumothorax, hemothorax and atelectasis: Pathology review
Chest X-ray interpretation: Clinical sciences
ECG axis
ECG basics
ECG cardiac hypertrophy and enlargement
ECG cardiac infarction and ischemia
ECG intervals
ECG normal sinus rhythm
ECG QRS transition
ECG rate and rhythm
Perioperative care
Anatomy of the gastrointestinal organs of the pelvis and perineum
Anatomy of the perineum
Anatomy of the vertebral canal
Bones of the vertebral column
Joints of the vertebral column
Vessels and nerves of the vertebral column
Anatomy clinical correlates: Spinal cord pathways
Anatomy clinical correlates: Vertebral canal
Blood components
Clot retraction and fibrinolysis
Coagulation (secondary hemostasis)
Platelet plug formation (primary hemostasis)
Acetaminophen (Paracetamol)
General anesthetics
Local anesthetics
Neuromuscular blockers
Non-steroidal anti-inflammatory drugs
Opioid agonists, mixed agonist-antagonists and partial agonists
Postoperative care
Cardiovascular system anatomy and physiology
Cytokines
Gastrointestinal system anatomy and physiology
Inflammation
Innate immune system
Introduction to the immune system
Lymphatic system anatomy and physiology
Nervous system anatomy and physiology
Regulation of pulmonary blood flow
Renal system anatomy and physiology
Respiratory system anatomy and physiology
Ventilation
Wound healing
Zones of pulmonary blood flow
Shock
Blood pressure, blood flow, and resistance
Carbon dioxide transport in blood
Cardiac afterload
Cardiac contractility
Cardiac cycle
Cardiac preload
Cardiac work
Changes in pressure-volume loops
Compliance of blood vessels
Frank-Starling relationship
Free radicals and cellular injury
Hypoxia
Ischemia
Law of Laplace
Measuring cardiac output (Fick principle)
Microcirculation and Starling forces
Oxygen binding capacity and oxygen content
Oxygen-hemoglobin dissociation curve
Pressure-volume loops
Pressures in the cardiovascular system
Stroke volume, ejection fraction, and cardiac output
Acid-base map and compensatory mechanisms
Buffering and Henderson-Hasselbalch equation
Physiologic pH and buffers
The role of the kidney in acid-base balance
Shock: Pathology review
Sympathomimetics: Direct agonists
Trauma
Anatomy of the abdominal viscera: Blood supply of the foregut, midgut and hindgut
Anatomy of the axilla
Anatomy of the pelvic cavity
Anatomy of the urinary organs of the pelvis
Anatomy of the vessels of the posterior abdominal wall
Arteries and veins of the pelvis
Deep structures of the neck: Root of the neck
Fascia, vessels and nerves of the upper limb
Introduction to the cranial nerves
Superficial structures of the neck: Anterior triangle
Superficial structures of the neck: Posterior triangle
Vessels and nerves of the forearm
Vessels and nerves of the gluteal region and posterior thigh
Vessels and nerves of the thoracic wall
Vessels and nerves of the vertebral column
Anatomy clinical correlates: Arm, elbow and forearm
Anatomy clinical correlates: Axilla
Anatomy clinical correlates: Bones, fascia and muscles of the neck
Anatomy clinical correlates: Cerebral hemispheres
Anatomy clinical correlates: Clavicle and shoulder
Anatomy clinical correlates: Eye
Anatomy clinical correlates: Female pelvis and perineum
Anatomy clinical correlates: Heart
Anatomy clinical correlates: Hip, gluteal region and thigh
Anatomy clinical correlates: Male pelvis and perineum
Anatomy clinical correlates: Mediastinum
Anatomy clinical correlates: Pleura and lungs
Anatomy clinical correlates: Skull, face and scalp
Anatomy clinical correlates: Spinal cord pathways
Anatomy clinical correlates: Thoracic wall
Anatomy clinical correlates: Vertebral canal
Anatomy clinical correlates: Vessels, nerves and lymphatics of the neck
Anatomy clinical correlates: Viscera of the neck
Anatomy clinical correlates: Wrist and hand
Eye conditions: Inflammation, infections and trauma: Pathology review
Pleural effusion, pneumothorax, hemothorax and atelectasis: Pathology review
Spinal cord disorders: Pathology review
Traumatic brain injury: Pathology review
Vomiting, diarrhea, and constipation
Anatomy of the abdominal viscera: Esophagus and stomach
Anatomy of the abdominal viscera: Large intestine
Anatomy of the abdominal viscera: Small intestine
Anatomy of the gastrointestinal organs of the pelvis and perineum
Anatomy clinical correlates: Viscera of the gastrointestinal tract
Colon histology
Small intestine histology
Stomach histology
Development of the digestive system and body cavities
Development of the gastrointestinal system
Gastrointestinal system anatomy and physiology
Appendicitis: Pathology review
Colorectal polyps and cancer: Pathology review
Diverticular disease: Pathology review
Gallbladder disorders: Pathology review
GERD, peptic ulcers, gastritis, and stomach cancer: Pathology review
Jaundice: Pathology review
Pancreatitis: Pathology review
Viral hepatitis: Pathology review
Communication of bad news
How to deliver bad news
Assessments
Opioid agonists, mixed agonist-antagonists and partial agonists
Flashcards
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Flashcards
Opioid agonists, mixed agonist-antagonists and partial agonists
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External References
First Aid
2022
2021
2020
2019
2018
2017
2016
Acetylcholine (ACh)
opioid analgesics p. 572
Acute pulmonary edema
opiod analgesics p. 572
Adverse effects/events
opioid analgesics p. 572
Calcium channels
opioid effect on p. 572
Diarrhea
opioids for p. 572
opioid withdrawal p. 594
5-HT
opioid effects p. 572
Glutamate
opioid effects p. 572
Heroin
opioids for withdrawal p. 572
Miosis
opioids p. 573
Naloxone
for opioid toxicity p. 249, 572, 594
Naltrexone
opioid toxicity p. 572, 594
Norepinephrine (NE)
opioid effect on p. 572
Opioids p. 573
Beers criteria p. 248
intoxication and withdrawal p. 594
pentazocine and p. 573
sleep apnea p. 703
toxicity treatment p. 249
Potassium channels
opioid effect p. 572
Pregnancy p. 657
opiate use during p. 639
Pulmonary edema
opioids for p. 572
Respiratory depression
opioids p. 573
Vomiting
with opioid analgesics p. 572
Transcript
Content Reviewers
Contributors
Opioid agonists are medications used mainly to control acute or chronic pain in particular situations.
Some of them are also used to treat diarrhea and cough. When treating pain, the goal should be to use short-acting opioids at the lowest effective dose for just a few days, and slowly increase their dose only as needed.
As a class, opioids share one thing in common, they bind to opioid receptors in the brain, spinal cord, and gastrointestinal tract.
Some are endogenous, meaning they are produced naturally by the body, like endorphins, short for endogenous morphine.
But others are exogenous, meaning they come from outside the body, like heroin and morphine, which come from the opium poppy; a flowering plant that oozes a milky white liquid.
To understand how opioids work, let’s zoom into a region of the brain tissue that has opioid receptors.
Normally, in the absence of endorphins, inhibitory neurons secrete a neurotransmitter called gamma-aminobutyric acid, or GABA, that prevents nearby neurons from releasing neurotransmitters like dopamine, serotonin, and norepinephrine.
Now, let’s say someone goes to play a rigorous game of badminton. Exercise releases endorphins which activate the three major opioid receptors located on the inhibitory neurons, called the mu, kappa, and delta receptors.
As endorphins bind to these receptors, they block the inhibitory neuron from releasing GABA, allowing the dopamine, serotonin, and norepinephrine secreting neurons to freely unload their neurotransmitters, which then get picked up by another neuron in the same area.
Norepinephrine and serotonin release takes place in pain processing regions of the brain like the thalamus, brainstem, and spinal cord, resulting in a decreased sensitivity to pain.
Summary
Opioid full agonists are drugs that bind to and activate opioid receptors in the body. They are used to treat pain and can also produce feelings of euphoria, which has led to their abuse and addiction potential. Examples of opioid agonists include morphine, codeine, and oxycodone.
Mixed agonist-antagonists bind to and activate opioid receptors to a certain extent, but also have the ability to block or inhibit the effects of other opioids. They can also be used to treat pain and may have a lower risk of abuse and addiction compared to full agonists.
Sources
- "Katzung & Trevor's Pharmacology Examination and Board Review,12th Edition" McGraw-Hill Education / Medical (2018)
- "Rang and Dale's Pharmacology" Elsevier (2019)
- "Behavioral Effects of Opioid Full and Partial Agonists During Chronic Buprenorphine Treatment" Journal of Pharmacology and Experimental Therapeutics (2019)
- "Opioid Use Disorder: Medical Treatment Options" Am Fam Physician (2019)
- "Primary care management of opioid use disorders: Abstinence, methadone, or buprenorphine-naloxone?" Can Fam Physician (2017)
- "Goodman and Gilman's The Pharmacological Basis of Therapeutics, 13th Edition" McGraw-Hill Education / Medical (2017)
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