Muscle Relaxants, Nonnarcotic Analgesics, Hormones & Topicals

Question 1

Muscle Relaxants

Answer 1

• 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

Question 2

Neuromuscular Blockers

Answer 2

• 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

Question 3

Spasmolytics

Answer 3

• 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

Question 4

baclofen

Answer 4

• another example of muscle relaxant
• used specifically for muscle spasticity resulting from:
  
  • mutiple sclerosis
  • cerebral palsy

Question 5

Non-narcotic Analgesics

Answer 5

used to reduce or remove the perception of pain

Question 6

Anti-inflammatory Drugs

Answer 6

• reduce the perception of pain

Question 7

NSAIDs

Answer 7

• Nonsteroidal Anti-inflammatory Drugs
• non-narcotic analgesic
• work to reduce the perception of pain
• examples:
  
  • ASA
  • ibuprofen
  • naproxen
  • indomethacin
  • ketorolac

Question 8

NSAID Action and Uses

Answer 8

• 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

Question 9

NSAID Side Effects

Answer 9

• GI and renal injuyr
• primairly - gastritis and ulcers

Question 10

COX-1 vs COX-2

Answer 10

• 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

Question 11

ASA

Answer 11

• 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

Question 12

Acetaminophen

Answer 12

• Tylenol®
• does have:
  
  • analgesic
  • antipyretic
• does not have:
  
  • anti-inflammatory
• Side Effects:
  
  • include fatal liver damage and should never be used with alcohol

Question 13

Rheumatoid Arthritis Drugs

Answer 13

• OTC anti-inflammatory agents can be used
• several drugs developed specifically for RA by inhibitng the activity of tumor necrosis factor:
  
  • adalimumab
  • etanercept
  • infliximab

Question 14

tumor necrosis factor

Answer 14

naturally occuring cytokine involved in normal inflammatory and immune response

Question 15

Hormones

Answer 15

• responsible for successful development and reproduction
• classes include:
  
  • adrenocortical hormones
  • sex steroids
  • thryoid
  • parathyroid
  • insulin
  • glucagon
  • hypoglycemic drugs

Question 16

Adrenocortical Hormones

Answer 16

• produced from adrenal cortex
• called adrenocorticosteroids and have
• 2 main groups
  
  • glucocorticoids
  • mineralcorticoids

Question 17

adrenal glands

Answer 17

• sit just above the kidneys
• inside the glands = adrenal cortex
  
  • responsible for production of steroids called adrenocorticosteroids

Question 18

Glucocorticoids

Answer 18

• 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

Question 19

glycogen

Answer 19

the main storage source of energy in animals

Question 20

Mineralocorticiods

Answer 20

• 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

Question 21

Sex Steroids

Answer 21

• produced by:
  
  • gonads
  • medulla of adrenal gland
• include:
  
  • estrogens
  • antiestrogens
  • progestin
  • antiprogestin
  • oral contraceptives
  • androgens
  • antiandrogens

Question 22

Estrogens

Answer 22

• primary female hormones
• include:
  
  • estradiol
    
    • ovary is primary source
  • estrone
  • estrioil
    
    • estradiol is converted into these two in the liver
• estrogen therapy is most commonly aimed at contraception and is combined with progestin to block ovulation to prevent pregnancy
• typical estrogen drugs:
  
  • diethylstilbestrol
  • estradiol

Question 23

Antiestrogens

Answer 23

• 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
      *

Question 24

Clomiphene

Answer 24

• 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

Question 25

Negative Feedback Cycle

Answer 25

a process in which a change from the normal range of function elicits a response that opposes or resists that change

Question 26

Progestin

Answer 26

• 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)

Question 27

Antiprogestins

Answer 27

• used in pregnancy termination
• main agent:
  
  • mifepristone
• works by breaking down the uterine lining which leads to an abortion

Question 28

Oral Contraceptives

Answer 28

• 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

Question 29

Androgen

Answer 29

• 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

Question 30

Antiandrogens

Answer 30

• used for:
  
  • excessive hair growth in women
  • prostate cancer in men
  • benign prostatic hypertrophy (BPH) = enlarged prostate
• examples include:
  
  • finasteride
  • dutasteride

Question 31

Thyroid Gland

Answer 31

• helps maintain metabolism
• 2 types:
  
  • hyperthyroidism (over active thyroid)
  • hypothyroidism (under active thyroid)

Question 32

Hyperthyroidism

Answer 32

• 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

Question 33

Hypothyroidism

Answer 33

• under active thyroid
• treated with hormone replacement therapy
  
  • levothyroxine

Question 34

PTH

Answer 34

• 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

Question 35

Hypoglycemic Drugs

Answer 35

*

Question 36

Type I Diabetes

Answer 36

• 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

Question 37

Type II Diabetes

Answer 37

• 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

Question 38

insulin

Answer 38

small protein that is destroyed by the acid of the stomach

must be administered by injection

Question 39

Sulfonylureas

Answer 39

• work by stimulating the release of insulin from the beta-cells in the pancreas which then reduces serum glucose levels
• agents:
  
  • glimepiride
  • glipizide
  • glyburide

Question 40

alpha-Glucosidase inhibitor

Answer 40

• agents:
  
  • acarbose
  • miglitol

Question 41

Thiazolidinedione

Answer 41

• (-glitazone)
• increase sensitivity to insulin by acting as agonists on a hormone receptor called PPAR-y = peroxisome proliferator activated receptor gamma
• agents:
  
  • rosiglitazone
  • pioglitazone

Question 42

Non-Sulfonylurea Secretagogues

Answer 42

• agents:
  
  • nateglinide
  • repaglinide

Question 43

Other Type II Oral agents

Answer 43

• metformin
  
  • works by increasing cellular insulin sensitivity
  • has a rare but potentially fatal side effect of lactic acidosis
• sitagliptin
• exenatide
• pramlintide

Question 44

Topical Medications

Answer 44

• 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
    *