Muscle Relaxants, Nonnarcotic Analgesics, Hormones & Topicals Flashcards
1
Q
Muscle Relaxants
A
- induce skeletal muscle relaxation by blocking neuromuscular function decreasing muscle tone
- work to combat muscle tension in a variety of disease states that can lead to movement problems and/or pain
- 2 major classes:
- neuromuscular blockers
- spasmolytics
2
Q
Neuromuscular Blockers
A
- work through interaction with the autonomic nervous system where they block the action of the chemical acetylcholine
- bind to nicotoinc receptors and work selectively
- used most often during surgery to make cutting through muscle easier
- examples inclued:
- succinylcholine
- atracurium
- cisatracurium
- pancuronium
3
Q
Spasmolytics
A
- work by inhibiting the neuronal signals in the motor neurons on muscles and reduce muscle contraction
- used for
- pain associated with muscle tension
- fibromyalgia
- tension headaches
- examples include:
- carisoprodol
- cyclobenzaprine
- metaxalone
- methocarbamol
4
Q
baclofen
A
- another example of muscle relaxant
- used specifically for muscle spasticity resulting from:
- mutiple sclerosis
- cerebral palsy
5
Q
Non-narcotic Analgesics
A
used to reduce or remove the perception of pain
6
Q
Anti-inflammatory Drugs
A
- reduce the perception of pain
7
Q
NSAIDs
A
- Nonsteroidal Anti-inflammatory Drugs
- non-narcotic analgesic
- work to reduce the perception of pain
- examples:
- ASA
- ibuprofen
- naproxen
- indomethacin
- ketorolac
8
Q
NSAID Action and Uses
A
- All NSAIDs work by inhibiting prostagladin synthesis by targeting the cyclooxgenase (COX) enzyme
- prostagladins modulate various components of inflammation and blocking COX enzyme leads to a reduction in inflammation
- have analgesic properties
- used as nonnarcotic pain reliever
- have antipyretic properties
- used as mild fever reducer
- also used for:
- tendinitis
- sunburn
- rheumatoid arthritis
- osteoarthritis
9
Q
NSAID Side Effects
A
- GI and renal injuyr
- primairly - gastritis and ulcers
10
Q
COX-1 vs COX-2
A
- COX enzyme exists in two forms
- COX-1
- COX-2
- COX-1
- expressed in most tissues
- thought to protect gastric mucosa - essential mucous in the GI tract
- COX-2
- expressed in brain and kidneys
- induced at site of inflammation
- selectively targeting COX-2 provides anti-inflammatory effect without harming the GI tract
- (-coxib) identivies COX-2 inhibitors
- celecoxib (Celebrex)
- etoricoxib
11
Q
ASA
A
- Aspirin
- non-narcotic analgesic
- also works on COX-1 and COX-2 enzymes by causing irreversible deactivation of the enzyme
- used as:
- anti-inflammatory agent
- analgesic
- heart attack preventative
- Heart attack preventative mechanism
- likely due to ASA inhibiting the production of thromboxane A2, leading to anticlotting action
12
Q
Acetaminophen
A
- Tylenol®
- does have:
- analgesic
- antipyretic
- does not have:
- anti-inflammatory
- Side Effects:
- include fatal liver damage and should never be used with alcohol
13
Q
Rheumatoid Arthritis Drugs
A
- OTC anti-inflammatory agents can be used
- several drugs developed specifically for RA by inhibitng the activity of tumor necrosis factor:
- adalimumab
- etanercept
- infliximab
14
Q
tumor necrosis factor
A
naturally occuring cytokine involved in normal inflammatory and immune response
15
Q
Hormones
A
- responsible for successful development and reproduction
- classes include:
- adrenocortical hormones
- sex steroids
- thryoid
- parathyroid
- insulin
- glucagon
- hypoglycemic drugs
16
Q
Adrenocortical Hormones
A
- produced from adrenal cortex
- called adrenocorticosteroids and have
- 2 main groups
- glucocorticoids
- mineralcorticoids
17
Q
adrenal glands
A
- sit just above the kidneys
- inside the glands = adrenal cortex
- responsible for production of steroids called adrenocorticosteroids
18
Q
Glucocorticoids
A
- have receptors throughout the body
- promote the breakdown of proteins
- involved in formation or generation of glucose (gluconeogenesis) leading to
- increased liver glycogen levels
- fasting blood-glucose levels
- urinary nitrogen output
- therapeutic basis:
- relates to their ability to inhibit inflammatory and immunological responses
- are used in:
- patients with malfunctioning adrenal glands
- main use is:
- reduce inflammation
- block immunological and/or allergic responses
- examples include:
- cortisone
- dexamethasone
- prednisone
- betamethasone
19
Q
glycogen
A
the main storage source of energy in animals
20
Q
Mineralocorticiods
A
- involved in salt and water balance
- increase the rate of sodium, bicarbonate and water reabsorption
- increase the rate of potassium secretion in kidney
- help maintain homeostasis of serum sodium and potassium levels
- commonly prescribed mineralcorticoid:
- fludrocortisone
21
Q
Sex Steroids
A
- produced by:
- gonads
- medulla of adrenal gland
- include:
- estrogens
- antiestrogens
- progestin
- antiprogestin
- oral contraceptives
- androgens
- antiandrogens
22
Q
Estrogens
A
- primary female hormones
- include:
- estradiol
- ovary is primary source
- estrone
- estrioil
- estradiol is converted into these two in the liver
- estradiol
- estrogen therapy is most commonly aimed at contraception and is combined with progestin to block ovulation to prevent pregnancy
- typical estrogen drugs:
- diethylstilbestrol
- estradiol
23
Q
Antiestrogens
A
- are antagonists to estrogen and block its action
- 2 important groups:
- SERMs = selective estrogen receptor modulators
- clomiphene
- typically, these drugs are used to treat diseases that are made worse by estrogen
- breast cancer
- examples:
- tamoxifen
- toremifene
- both used to treat breast cancer
*
- both used to treat breast cancer
24
Q
Clomiphene
A
- an antiestrogen that stimulates ovarian production
- used in treatment of infertility
- acts by functioning as estrogen receptor antagonist in the hypothalamus and interfering with the inhibitory feedback of estrogen
- is a negative feedback cycle so it results in an increased release of gonadotropin-releasing hormone
- the gonadotropin then stimulates the ovulation
25
Negative Feedback Cycle
a process in which a change from the normal range of function elicits a response that opposes or resists that change
26
Progestin
* progesterone is the main natural progestin
* used as:
* oral contraceptive
* therapeutic drug
* it serves in the role of maintaining the uterine endometrium during pregnancy
* side effects:
* weight gain
* depression
* edema (swelling)
27
Antiprogestins
* used in pregnancy termination
* main agent:
* mifepristone
* works by breaking down the uterine lining which leads to an abortion
28
Oral Contraceptives
* estrogen and progestin
* complete mechanism is not understood
* side effects:
* nausea
* vomiting
* depression
* edema
* increased risk of abnormal clotting in women over 35 who smoke
29
Androgen
* group of hormones that has a masculinizing and weight gain (anabolic) effect
* works in both men and women
* drug effects include:
* increased muscle mass
* increased bone density
* increased red blood cell mass
* Testosterone
* is the major androgen produced in the body
* Therapeutic use
* testicular deficiency
* Side effects:
* impotence
* decreased sperm production
* enlarged breasts (gynecomastia)
* liver abnormalities
* psychotic episodes
30
Antiandrogens
* used for:
* excessive hair growth in women
* prostate cancer in men
* benign prostatic hypertrophy (BPH) = enlarged prostate
* examples include:
* finasteride
* dutasteride
31
Thyroid Gland
* helps maintain metabolism
* 2 types:
* hyperthyroidism (over active thyroid)
* hypothyroidism (under active thyroid)
32
Hyperthyroidism
* overactive thyroid
* treated with:
* surgery or radioactive iodine to remove part of all of the thyroid gland - thyroid hormone levels are then maintained through hypothyroid treatment if needed
* drugs can also be used that inhibit thyroid hormone synthesis:
* propylthiouracil
* methimazol
33
Hypothyroidism
* under active thyroid
* treated with hormone replacement therapy
* levothyroxine
34
PTH
* parathyroid hormone
* most important regulator of calcium homeostasis
* effect in kidneys:
* PTH is secreted by parathyroid gland and acts on the kidneys to produce and increased reabsorption rate of calcium
* effect on bones:
* calcium reabsorption produces increased bone mass
* disregulation of PTH
* osteoporosis
* treated with:
* teriparatide
* recombinant form of PTH
35
Hypoglycemic Drugs
*
36
Type I Diabetes
* insulin dependent
* related to loss of insulin secreting cells in the pancreas
* Type I diabetics need a source of insulin that is supplied to them
* usually by injection
37
Type II Diabetes
* non insulin dependent
* related to cell resistance to the action of insulin
* typically treated with oral drugs that lower blood glucose
* also treated with insulin
* goal of treatment is to lower blood glucose
* 5 classes of oral agents:
* sulfonylureas
* alpha-glucosidase inhibitor
* thiazolidinedione
* non-sulfonylurea secretagogues
* other
38
insulin
small protein that is destroyed by the acid of the stomach
must be administered by injection
39
Sulfonylureas
* work by stimulating the release of insulin from the beta-cells in the pancreas which then reduces serum glucose levels
* agents:
* glimepiride
* glipizide
* glyburide
40
alpha-Glucosidase inhibitor
* agents:
* acarbose
* miglitol
41
Thiazolidinedione
* (-glitazone)
* increase sensitivity to insulin by acting as agonists on a hormone receptor called PPAR-y = peroxisome proliferator activated receptor gamma
* agents:
* rosiglitazone
* pioglitazone
42
Non-Sulfonylurea Secretagogues
* agents:
* nateglinide
* repaglinide
43
Other Type II Oral agents
* metformin
* works by increasing cellular insulin sensitivity
* has a rare but potentially fatal side effect of lactic acidosis
* sitagliptin
* exenatide
* pramlintide
44
Topical Medications
* forms:
* creams
* ointments
* gels
* lotions
* applied to the surface of skin or other organs (ex. eyes, gums, teeth, nose, ears & lungs through inhalation)
* topical application of drugs avoids the liver (hepatic processing)
* some medications are highly metabolized by the liver and can cause liver damage (ex. testosterone) making topical route the best form of administration for these medications
* also sustained delivery of drugs is possible through topical administration
* ex. ortho evra - topical administration of contraceptive
*
