Pharmacology: Review of 13, 18, 31
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The "fight or flight" response refers to the set of actions that occur when the _____ nervous system is activated.
What are the two primary neurotransmitters of the autonomic nervous system?
Norepinephrine and Acetylcholine
What is the neurotransmitter released at almost all postganglionic nerves in the sympathetic nervous system? What is the exception?
- Sweat glands (acetylcholine is released)
____ drugs stimulate the sympathetic nervous system.
_____ drugs inhibit the sympathetic nervous system.
Sympatholytics, aka adrenergic agonists
What two types of cholinergic receptors exist in the nervous system?
- Nicotinic Receptors
- Muscarinic Receptors
_____ receptors are acetylcholine receptors that are present in the skeletal muscle, which is controlled by the somatic nervous system.
What is the main acetylcholine postganglionic receptor of the autonomic nervous system?
These drugs stimulate the parasympathetic nervous system.
Cholinergics, aka parasympathomimetics
These drugs inhibit the parasympathetic nervous system.
Anricholinergics, aka parasympatholytics, muscarinic blockers
If a drug is said to have anticholinergic side effects, what sort of side effects can a patient expect to have (7)?
- Dry mouth
- Dry eyes
- Difficulty urinating
- Dry skin (inability to perspire)
- Increased heart rate
Alpha2 Adrenergic receptors are located where? What is their response to stimulation by norepinephrine?
- Presynaptic adrenergic nerve terminals
- Inhibition of the release of norepinephrine
Alpha1 Adrenergic receptors are located where? What is their response to stimulation by norepinephrine?
- All sympathetic target organs EXCEPT the heart
- Constriction of blood vessels, dilation of pupils
Beta1 adrenergic receptors are located where? What is their response to stimulation by norepinephrine?
- Heart and Kidneys
- Increased heart rate and force of contraction; release of renin
Beta2 Adrenergic receptors are located where? What is their response to stimulation by norepinephrine?
- All sympathetic target organs EXCEPT the heart
- Inhibition of smooth muscle
Sympathomimetics that stimulate Alpha1 receptors will produce what actions?
- Treatment of nasal congestion and hypotension
- Causes mydriasis during opthalamic examinations
Sympathomimetics that stimulate Alpha2 receptors will produce what effects?
Treatment of hypertension through a centrally acting mechanism (b/c stimulation of these receptors reduces norepinephrine release).
Sympathomimetics that stimulate Beta1 receptors will have what sort of effects?
- Treatment of cardiac arrest, heart failure, and shock
- (Increased heart rate and force of contraction, release of renin)
Sympathomimetics that stimulate Beta2 receptors produce what effects?
- Treatment of Asthma and premature labor contractions
- (inhibition of smooth muscle)
The endogenous sympathomimetic ______ stimulates all four types of adrenergic receptors. What pharmacological use does this have?
- Cardiac arrest and asthma
The side effects of sympathomimetics are mostly extensions of their ______ actions. Give examples of these side effects.
- Tachycardia, hypertension, dysrhythmia
- CNS excitement
Pain may be classified according to its _______.
_____ pain results from injury to tissues. This type of pain is often described as somatic or visceral. What descriptors are often attached to this kind of pain?
- Sharp, localized (somatic)
- Generalized, dull, throbbing, or aching (visceral)
____ pain results from injury to the nerves and is typically described how by patients?
- Burning, shooting, numb
Sharp, localized sensations of pain.
Somatic pain (a type of nociceptive pain)
Generalized dull, throbbing, or aching sensations
Visceral pain (a type of nociceptive pain)
Acupuncture, biofeedback, and massage are all examples of ____ pain management treatments.
The process of pain transmission begins when pain receptors, called _____ are stimulated.
The nerve impulses signaling pain are sent to the spinal cord bby way of two types of sensory neurons. What are they?
Asigma and C fibers
____ fibers are myelinated and send sharp, well defined pain whereas ____ fibers are unmyelinated and conduct dull, poorly localized pain.
Once pain impulses reach the spinal cord, neurotransmitters are responsible for transmitting the message along to the next set of neurons: a neurotransmitter called _____ is thought to be responsible for continuing the message.
____ are thought to modify sensory information by influencing the activity of substance P.
In general, two main classes of pain medications are employed to manage pain. What are they? Where do they act?
- Opoids: act within the CNS
- NSAIDs: act at the peripheral tissue level
____ are medications that are used to relieve pain.
____ are narcotic substances responsible for reducing moderate to severe pain.
____ is a general term often used to describe opiod drugs that produce analgesia and CNS depression.
Narcotics (produce numbness and stupor like symptoms)
In common usage a ____ is the same as an opiod, and the terms are often used interchangeably.
From the perspective of pain management, what are the two important receptors that opioids stimulate?
____ are the first line of choice for moderate to severe pain
Opioids, aka opioid agonists
By using _______, patients are allowed to self medicate with opiate medication by the pressing of a button. Safe levels of scheduled medication are delivered with an infusion pump.
PCA, patient controlled analgesia
In the pharmacologic management of pain, it is common practice to combine opioids and _____ into a single tablet or capsule. Why is this method used?
- nonnarcotic analgesics
- The two classes of analgesics work synergistically to relieve pain
- The dose of the opioid can be kept small to avoid dependance and narcotic related side effects.
_____ are substances that prevent the effects of opoiod agonists.
What may be used to reverse the symptoms of opioid addiction, toxicity, and overdose?
Sedation and respiratory distress are both symptoms of _____ toxicity. What is used to treat this?
- Opioid toxicity.
- Opioid antagonists
Infusion with the opioid antagonist _____ may be used to reverse respiratory distress and other acute symptoms of opioid toxicity.
In cases in which a patient is unconscious or it is unclear what drug has been taken, what may be given in order to diagnose an opioid overdose? How?
- naloxone (Narcan), an opioid antagonist.
- If the opioid antagonist fails to quickly reverse the acute symptoms, the overdose ma be attributed to a nonopioid substance.
What are early symptoms of opioid withdrawl (8)?
- Muscle aches
- Increased tearing
- Runny nose
What are the more severe, late symptoms of opioid withdrawl (7)?
- Mood changes
- Muscle spasms
- Extreme irritiability
The nonopioid analgesics include _____, _____, and a few cenrally acting drugs.
The ____ act by inhibiting pain mediators at the nociceptor level. When tissue is damaged, chemical mediators are released locally. What are they?
- Potassium and hydrogen ions
The chemical mediator____ is associated with the sensory impulse of pain, while ____ can induce pain through the formation of free radicals.
NSAIDs work by inhibiting _____, an enzyme responsible to the formation of prostaglandins. What are the effects of inhibiting this enzyme?
inflammation and pain are reduced
____ are the drugs of choices for mild to moderate pain, especially pain associated with inflammation.
What properties do NSAIDs possess that make them more advantageous and versatile than opioids?
they have antipyretic and anti-inflammatory activity in addition to their analgesic properties
_____ reduces fever by direct action at the level of the hypothalamus and causes dilation of the peripheral blood vessels enabling sweating and dissipation of heat.
____ is the primary alternative to NSAIDs when patients cannot take aspirin or ibuprofen. Why?
- It does not cause GI bleeding or ulcers
- It does not exhibit cardiotoxicity
- It has similar efficacies in relieving pain and reducing fever.
Does Acetaminophen have anti-inflammatory properties?
What is the main adverse effect of Tylenol?
The risk for liver damage (hepatotoxicity)
Hepatotoxicity is associated with______ while renal toxicity is associated with ______.
The most painful type of headache is the ___a__, which is characterized by throbbing or pulsating pain, sometimes preceded by auras-- sensory cues that let you know that a migraine headache is coming soon. Most __a__ are accompanied by what GI symptoms?
- nausea and vomitting
What are the two major classes of drugs that are used as antimigraine drugs? What do they have in common?
- The Triptans
- The Ergot Alkaloids
- Both are serotonin (5-HT) agonists
Pharmacotherapy of migraine headaches generally begins with _____________. If the migraine headaches persist, what are the drugs of choice?
- Acetaminophen or NSAIDs
These drugs are selective for the 5-HT1-receptor subtype, and they are though to act by constricting certain intracranial vessels. Are they used for migraine abortion or prophylaxis?
- Abortion (with or without auras)
For migraine patients who are unresponsive to the triptans, what drugs may be used to abort migraines?
What drug classes are used for migraine prophylaxis? When is prophylaxis of migraines initiated?
- Antiseizure drugs
- Beta blockers
- Calcium Channel blockers
Prophylaxis is initiated only if the incidence of migraines is high and the patient is unresponsive to drugs used to abort migraines.
What is the most commonly prescribed drug class for the prophylaxis of migraines?
True or False: Prophylactic treatment for migraines is initiated once an effective abortive drug has been found.
False: If the patient responds to drugs that abort migraines, no prophylaxis is needed unless the incidence of migraines is high.
_____ is specific to the synthesis of inflammatory prostaglandins and is the basis of NSAID therapy. What is responsible for the GI bleeding associated with NSAID therapy?
Inhibition of COX-1
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