Antiretroviral formulations for adults unable to swallow tablets/capsules

Options for those unable to swallow tablets/capsules	Antiretroviral agents^*
Oral liquid formulation available	NRTI:^¶ Abacavir (20 mg/mL), emtricitabine (10 mg/mL), lamivudine (10 mg/mL), zidovudine (10 mg/mL).
	NNRTI: Nevirapine (10 mg/mL).
	PI: Darunavir (100 mg/mL), fosamprenavir (50 mg/mL), lopinavir-ritonavir (80 mg lopinavir and 20 mg ritonavir per mL)^Δ, tipranavir (100 mg/mL).
	CCR5 antagonist: Maraviroc (20 mg/mL).
	Pharmacokinetic enhancer: Ritonavir (80 mg/mL).^Δ
Powder packet granules, or chewable tablet formulation available	NRTI: Tenofovir disoproxil fumarate (TDF) powder granules for mixture with soft foods (40 mg TDF per scoop; for adults, this requires 7.5 scoops per dose).
	PI: Atazanavir (50 mg oral powder for mixture with beverages or soft foods), ritonavir (100 mg oral power for mixture with soft foods).
	INSTI: Raltegravir (chewable tablets [25 and 100 mg] and packet for oral suspension [100 mg/5 mL reconstituted).^◊
Tablets can be dissolved or dispersed in liquid^§	NNRTI: Etravirine (tablet may be dispersed in water).
Tablets can be dissolved or dispersed in liquid^§	PI: Nelfinavir (tablet may be crushed or dissolved).
Tablets can be crushed; capsules can be opened^¥	NRTI: Emtricitabine (capsule may be opened), lamivudine (tablet may be crushed), tenofovir disoproxil fumarate (tablet may be crushed).
	NNRTI: Efavirenz (capsules may be opened).^‡
	PI: Darunavir (tablet may be crushed), nelfinavir (tablet may be crushed or dissolved), saquinavir (capsule may be opened).
	INSTI: Bictegravir-emtricitabine-tenofovir alafenamide, dolutegravir, elvitegravir-cobicistat-emtricitabine-tenofovir disoproxil fumarate.
Tablets can be crushed and administered via gastrostomy or nasogastric tubes^†	NRTI: Tenofovir disoproxil fumarate, emtricitabine.
	NNRTI: Etravirine.
	INSTI: Raltegravir, elvitegravir-cobicistat-emtricitabine-tenofovir disoproxil fumarate.
Tablets are very small, easy to swallow	Rilpivirine.
	Dolutegravir.
	Tenofovir alafenamide-emtricitabine.
	Rilpivirine-emtricitabine-tenofovir alafenamide.
	Bictegravir-emtricitabine-tenofovir alafenamide.
Tablets that should not be crushed or dissolved	Lopinavir-ritonavir tablets.
	Efavirenz-emtricitabine-tenofovir disoproxil fumarate coformulation.
	Nevirapine extended-release.
	Ritonavir tablets.
	Darunavir-cobicistat tablets and atazanavir-cobicistat tablets.
Injectable formulations available	Enfuvirtide (subcutaneous injection twice daily).
Injectable formulations available	Zidovudine (intravenous).
Components of coformulations may be available as separate drugs in liquid or powder form	Efavirenz-emtricitabine-tenofovir disoproxil fumarate.^‡
	Rilpivirine-tenofovir disoproxil fumarate-emtricitabine: Rilpivirine tablet very small, but no liquid option available. Tenofovir disoproxil fumarate powder and emtricitabine liquid available separately.
	Zidovudine-lamivudine: Liquid formulation for each component available separately.
	Zidovudine-lamivudine-abacavir: Liquid formulation for each component available separately.
	Tenofovir disoproxil fumarate-emtricitabine: Tenofovir powder and emtricitabine liquid available separately.
	Abacavir-lamivudine: Liquid formulation for each component available separately.
	Lopinavir-ritonavir: Coformulated liquid available.

NRTI: nucleoside/nucleotide reverse transcriptase inhibitors; NNRTI: non-nucleoside reverse transcriptase inhibitors; PI: protease inhibitors; INSTI: integrase inhibitors.
* Administration detail of antiretroviral preparations listed in this table refer to products available in the United States, Canada, and some other countries. Refer to the Lexicomp individual drug monographs included within UpToDate and local product labeling for additional information.
¶ Didanosine and stavudine are available as powder for oral suspension; however, these agents are rarely used because of toxicity.
Δ Liquid formulation available but not very palatable for most adults. These formulations should not be used with polyurethane feeding tubes.
◊ Not bioequivalent to the adult film coated tablet. Refer to Lexicomp drug information topic for dosing.
§ Good instructions and relatively good bioavailability data available.
¥ To be prepared immediately before ingestion. Instructions available but little to no stability or bioavailability data available.
‡ The efavirenz capsules can be opened; however, the tablets should not be crushed.
† Minimal data from case reports.

References:

Nyberg CR, Patterson BY, Williams MM. When patients cannot take pills: Antiretroviral drug formulations for managing adult HIV infection topics. Top Antivir Med 2011; 19:126.
Swindells S, Flexner C, Fletcher CV, Jacobson JM. The critical need for alternative antiretroviral formulations and obstacles to their development. J Infect Dis 2011; 204:669.
Hoon M, Colbers A,Burger DM et al, et al. Pharmacokinetics of crushed elvitegravir combination tablet given with drip feed. Presented at the Conference on Retroviruses and Opportunistic Infections. Boston. 2016.
Bristol-Myers Squibb Canada. Our Key Products. http://www.bmscanada.ca/en/products/evotaz (Accessed on May 10, 2016).

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Antiretroviral formulations for adults unable to swallow tablets/capsules