SUPPOSOTORIES, INSERTS, AND STICKS

Suppositories

These are solid dosage forms intended for insertion into body orifices where they melt, soften, or dissolve and exert local or systemic effects.

Suppositories

One or more APIs are dispersed in a suitable base and molded or otherwise formed into a suitable shape for insertion into the rectum.

False (one or more APIs are dispersed)

True or False:

Only one API is dispersed in a suitable base and molded or otherwise formed into a suitable shape for insertion into the rectum.

Suppositories

It is intended to be absorbed into the general circulation to provide systemic effects.

general circulation; systemic effects

It is intended to be absorbed into the __________________ to provide _________________.

rectal route

The ____________________ of administration is especially useful if the patient is unwilling or unable to take medication by mouth.

Supponere

It is a Latin word that means “to place under“ in which suppositories has been derived.

1. Promote defecation

2. Introduce drugs into the body

3. Treat anorectal diseases 

Suppositories are employed for 3 reasons:

1%

In the United States, how many percent of the drugs are formulated as suppositories?

5%

In Germany, how many percent of the drugs are formulated as suppositories?

• Relatively Low Cost

• Lack of Technical Difficulties

Why is rectal drug administration attractive compared to parenteral therapy?

• Esthetics and Stigma of Violating the Patient’s Dignity

• Potential Rectal Irritation due to frequent administration

• Difficulty in titrating a correct dose due to limited strengths of commercial suppositories

What are the downside and challenges of rectal administration?

Suppositories

They are a dosage form that can be administered to avoid nausea and vomiting caused by certain medications upon oral administration.

Suppositories

It is a dosage form that can often result in a fast onset of action.

1. Position the patient on the left side with the upper leg flexed.

2. Lubricate the suppository with a water-soluble lubricant or a small amount of water, if needed.

3. Gently insert the suppository in the rectum a finger’s depth at an angle toward the umbilicus, so the suppository is placed against the rectal wall for absorption, rather than being left in the canal or pushed into a mass of stool.

4. After the finger is withdrawn, hold the buttocks together until the urge to expel has ceased.

How to use a suppository?

Patient should be on the left side with the upper leg flexed

What should be the position when inserting suppository?

water-soluble lubricant or a small amount of water

What is used to lubricate the suppository when inserting it?

• Finger’s depth

• Angle toward the umbilicus

What is the depth and angle when suppository is inserted?

Rectal Wall

Where is suppository placed when inserted?

In the Refrigerator

Where should suppositories be stored?

True

True or False:

Suppositories, if they must be stored in the refrigerator, should be allowed to warm to room temperature before insertion.

False (allowed to warm to room temperature)

True or False:

Suppositories, if they must be stored in the refrigerator, should not be allowed to warm to room temperature before insertion.

cocoa butter suppositories

Rub ________________________ gently with the fingers to melt the surface to provide lubrication for insertion. 

Glycerinated gelatin or polyethylene glycol suppositories

______________________________________________________ should be moistened with water to enhance lubrication. 

False (they are inserted with the aid of an appliance)

True or False:

Vaginal inserts are inserted with fingers.

True

True or False:

Rectal suppositories are inserted with fingers.

32 mm or 1.5 inches

What is the length of rectal suppositories?

• cylindrical with one or both ends tapered;

• bullet, torpedo, 

• little finger

What are the shapes of rectal suppository?

2 grams

What is the weight of adult rectal suppository when cocoa butter is employed as base?

Pencil-like shape

What is the shape used for child suppository?

weighs half as adult suppositories

What is the weight of a child’s suppository?

Suppositories or Pessaries

What is the other name or former name of vaginal inserts?

• globular

• oviform

• cone-shaped

What are the shapes used in vaginal inserts?

5 grams

What is the weight of vaginal inserts when cocoa butter base is used?

Bougies

What is the other name for urethral inserts?

• Slender

• pencil-shaped

What are the shapes of urethral inserts?

3 to 6 mm

What is the diameter of male urethral suppositories?

140 mm

What is the length of a male urethral suppository?

4 g

What is the weight of a male urethral suppository when cocoa butter base is employed>?

70 mm

What is the length of a female urethral suppository?

2 g

What is the weight of a female urethral suppository when cocoa butter base is employed?

5 g to 25 g

What is the weight range of medication sticks?

cylindrical

What is the shape of medication sticks?

• Applicator Tube (Topical Administration)

• Applicator

What is generally packaged with medication sticks?

• Aspirin and Opiates - Pain

• Ergotamine tartrate - Migraine Headaches

• Theophylline 

• Chlorpromazine 

• Bisacodyl

What are examples of suppositories?

1. First-pass effect: 

2. Drug stability: 

3. Large dose drugs: 

4. Irritating drugs: 

5. Unpleasant tasting or smelling drugs:

6. In children, the rectal route is especially useful. 

7. In patients experiencing nausea and vomiting or when the patient is unconscious.

8. The presence of disease of the upper gastrointestinal tract that may interfere with drug absorption.

9. Objectionable taste or odor of a drug

10. Achievement of a rapid drug effect systemically

What are the advantages of rectal administration?

Drug Stability

Advantages of Rectal Administration:

• Avoiding the breakdown of certain drugs that are susceptible to gastric degradation.

Large dose drugs

Advantages of Rectal Administration:

• Ability to administer somewhat larger doses of drugs than using oral administration.

First-pass effect

Advantages of Rectal Administration:

• Avoiding, at least partially, the _________________ that may result in higher blood levels for those drugs subject to extensive first-pass metabolism upon oral administration.

Irritating drugs

Advantages of Rectal Administration:

• Ability to administer drugs that may have an irritating effect on the oral or gastrointestinal mucosa when administered orally.

Unpleasant tasting or smelling drugs

Advantages of Rectal Administration:

• Ability to administer unpleasant tasting or smelling drugs whose oral administration is limited.

In children, the rectal route is especially useful.

Advantages of Rectal Administration:

• An ill child may refuse oral medication and may fear injections.

1. A perceived lack of flexibility regarding the dosage of commercially available suppositories resulting in underuse and a lack of availability.

2. If suppositories are made on demand they may be expensive.

3. Suppositories as a dosage form are safe, but they exhibit variable effectiveness.

4. Different formulations of a drug with a narrow therapeutic margin, such as aminophylline, cannot be interchanged without risk of toxicity.

5. The “bullet-shaped” suppository after insertion can leave the anorectal site and ascend to the rectosigmoid and descending colon. Hence, one may consider that suppositories with this shape possibly should not be used at bedtime.

6. Defecation may interrupt the absorption process of the drug; this may especially occur if the drug is irritating.

7. The absorbing surface area of the rectum is much smaller than that of the small intestine.

8. The fluid content of the rectum is much less than that of the small intestine, which may affect the dissolution rate, etc.

9. There is the possibility of degradation of some drugs by the microflora present in the rectum.

10. The dose of a drug required for rectal administration may be greater than or less than the dose of the same drug given orally. 

What are the disadvantages of suppositories?

point-end first

Bullet-shaped rectal suppositories should be inserted __________________.

half lengthwise

If instructed to use a one-half suppository, cut the suppository in ____________________ with a clean razor blade.

• rapidity

• intensity

• duration of action

3 parameters that must be considered during formulation for rectal administration:

Glycerin Suppositories

• This product is used to relieve occasional constipation.

Glycerin

It belongs to a class of drugs known as hyperosmotic laxatives.

Glycerin Suppositories

It works by drawing water into the intestines. This effect usually results in a bowel movement within 15 to 60 minutes.

Glycerin Suppositories

Packaged in tightly closed glass containers to prevent a change in moisture content.

15 to 60 minutes

How long does glycerin suppositories take effect on one’s bowel movement?

Inserts

It is a solid dosage form that is inserted into a naturally occurring (nonsurgical) body cavity other than the mouth or rectum, including the vagina and urethra,  where drugs are released, generally for localized effects.

Vaginal inserts

Formerly called pessaries

Vaginal inserts

Preparations are employed principally to combat infections in the female genitourinary tract, to restore the vaginal mucosa to its normal state, and for contraception.

polyethylene glycols

The most commonly used base for vaginal inserts consists of combinations of various molecular weight ___________________.

Parabens

Commonly added surfactants and preservative agents.

 acid pH usually about 4.5

Many vaginal inserts and other types of vaginal dosage forms are buffered to this pH consistent with the normal vagina.

Vaginal inserts

They are widely used today as they are easy to manufacture, more stable, and less messy. 

Vaginal inserts

They are usually ovoid and are accompanied in their packaging with a plastic inserter.

Urethral inserts

also called bougies,

Urethral inserts

These are slender, pencil-shaped suppositories intended for insertion into the male or female urethra.

The MUSE (alprostadil) urethral micro suppository (Vivus, Inc.)

It is a single-use medicated transurethral system for the delivery of alprostadil to the male urethra.

The MUSE (alprostadil) urethral micro suppository (Vivus, Inc.)

It is indicated for the treatment of erectile dysfunction.

Sticks

They are generally packaged in an applicator tube for topical administration, and the applicator can be adjusted to continually expose new, fresh stick from inside the tube.

Sticks

It provides pharmacists, patients, and primary care providers with a unique, convenient, relatively stable, easy-to-prepare dosage form for the topical delivery of drugs.

Sticks

These are prepared similar to suppositories except that the melt is poured into the administering device, or tube. 

• the stick is pushed up from the bottom

• a screw-type device to raise the stick

Application of sticks.

True

True of False:

The patient should be told to apply the stick only to the involved area and not to the surrounding skin.

False (not to the surrounding skin)

True of False:

The patient should be told to apply the stick only to the involved area and to the surrounding skin.

False (only as needed)

True or False:

The patient should apply the medication liberally over the area every 4 hours.

True

True or False:

To avoid transmitting infection, the product should not be shared with others.

True

True or False:

The surface of the stick should be cleaned with a clean tissue after each use.

• (a) anatomic and physiologic factors and 

• (b) physicochemical factors of the drug and the base.

The factors that affect the rectal absorption of a drug administered in the form of a suppository.

rectum, terminating as the anus 

The last few inches of the large intestine.

• Superior hemorrhoidal vein 

• Middle hemorrhoidal vein 

• Inferior hemorrhoidal vein 

Rectum contains three types of hemorrhoidal veins 

Hemorrhoidal Veins

Act by transporting the active principle absorbed in the rectum to the blood system either directly or indirectly.

anastomosis network

What links the three hemorrhoidal veins?

At least 50% to 70%

___________________ of the active ingredients administered rectally take the direct pathway.

lymphatic vessels

There is also the possibility of absorption into the ____________________________ that should not be dismissed but may be minimal. 

Direct transport

By means of iliac veins and the vena cava (inferior and middle hemorrhoidal veins)

Indirect transport

By means of the portal vein and the liver

1. Circulation Route 

2. pH and lack of buffering capacity of the rectal fluids 

3. Colonic Content

Physiological factors affecting rectal drug absorption.

Circulation Route

• Drugs absorbed rectally can bypass the portal circulation during their first pass into the general circulation.

• This enables drugs that are otherwise destroyed in the liver to exert systemic effects. 

Circulation Route

• The lower hemorrhoidal veins surrounding the colon receive the absorbed drug and initiate its circulation throughout the body, bypassing the liver. 

Circulation Route

Lymphatic circulation also assists in the absorption of rectally administered drugs.

7.2 to 7.4

The pH of the rectal fluid is generally in the range of _______________, and it has negligible buffer capacity. 

pH and lack of buffering capacity of the rectal fluids

• The form in which the drug is administered will not generally be chemically changed by the rectal environment; therefore, the pH of the medium may be determined by the characteristics of the drug. medium may be determined by the characteristics of the drug

Colonic Content

• A drug will obviously have a greater opportunity to make contact with the absorbing surface of the rectum and colon in the absence of fecal matter. 

Colonic Content

• An evacuant enema may be administered and allowed to act before the administration of a suppository of a drug to be absorbed.

Colonic Content

• Other conditions such as diarrhea, colonic obstruction due to tumorous growths, and tissue dehydration can all influence the rate and degree of drug absorption from the rectal site.